346 articles for thisTarget
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Green synthesis of novel spiro-indenoquinoxaline derivatives and their cholinesterases inhibition activity.
Persian Gulf University
Design, synthesis and biological evaluation of bambuterol analogues as novel inhibitors of butyrylcholinesterase.
South China University Of Technology
Tacrine-resveratrol fused hybrids as multi-target-directed ligands against Alzheimer's disease.
University Of Bologna
A review on tacrine-based scaffolds as multi-target drugs (MTDLs) for Alzheimer's disease.
Tehran University Of Medical Sciences
2,4-Disubstituted quinazolines as amyloid-ß aggregation inhibitors with dual cholinesterase inhibition and antioxidant properties: Development and structure-activity relationship (SAR) studies.
University Of Waterloo
Aurone Mannich base derivatives as promising multifunctional agents with acetylcholinesterase inhibition, anti-ß-amyloid aggragation and neuroprotective properties for the treatment of Alzheimer's disease.
Sichuan University
Amino derivatives of platanic acid act as selective and potent inhibitors of butyrylcholinesterase.
Martin-Luther-University Halle-Wittenberg
Tetrahydropyranodiquinolin-8-amines as new, non hepatotoxic, antioxidant, and acetylcholinesterase inhibitors for Alzheimer's disease therapy.
University Of Sfax
Novel ferulic amide derivatives with tertiary amine side chain as acetylcholinesterase and butyrylcholinesterase inhibitors: The influence of carbon spacer length, alkylamine and aromatic group.
Hu'Nan University
Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation.
Jagiellonian University Medical College
New azepino[4,3-b]indole derivatives as nanomolar selective inhibitors of human butyrylcholinesterase showing protective effects against NMDA-induced neurotoxicity.
University Of Bari&Quot;A. Moro&Quot
Neurodegenerative diseases linked to misfolded proteins and their therapeutic approaches: A review.
Aligarh Muslim University
Novel multi-target-directed ligands for Alzheimer's disease: Combining cholinesterase inhibitors and 5-HT
Jagiellonian University Collegium Medicum
Design and synthesis of new piperidone grafted acetylcholinesterase inhibitors.
University Of Nebraska Medical Center
Rational modification of donepezil as multifunctional acetylcholinesterase inhibitors for the treatment of Alzheimer's disease.
China Pharmaceutical University
Design, synthesis, biological evaluation, and molecular modeling studies of chalcone-rivastigmine hybrids as cholinesterase inhibitors.
South China University Of Technology
Synthesis, structure-activity relationship and molecular docking of 3-oxoaurones and 3-thioaurones as acetylcholinesterase and butyrylcholinesterase inhibitors.
University Of Gujrat
Discovery of Selective Inhibitors Targeting Acetylcholinesterase 1 from Disease-Transmitting Mosquitoes.
Ume£
Donepezil-like multifunctional agents: Design, synthesis, molecular modeling and biological evaluation.
Okayama University
New cinnamic - N-benzylpiperidine and cinnamic - N,N-dibenzyl(N-methyl)amine hybrids as Alzheimer-directed multitarget drugs with antioxidant, cholinergic, neuroprotective and neurogenic properties.
Instituto De Qu£Mica M£Dica
Novel potent pyridoxine-based inhibitors of AChE and BChE, structural analogs of pyridostigmine, with improved in vivo safety profile.
Kazan (Volga Region) Federal University
Fatty Acid Amide Hydrolase (FAAH), Acetylcholinesterase (AChE), and Butyrylcholinesterase (BuChE): Networked Targets for the Development of Carbamates as Potential Anti-Alzheimer's Disease Agents.
Alma Mater Studiorum-University Of Bologna
Synthesis and in vitro reactivation study of isonicotinamide derivatives of 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide as reactivators of Sarin and VX inhibited human acetylcholinesterase (hAChE).
Defence Research & Development Establishment
Synthesis and evaluation of multi-target-directed ligands for the treatment of Alzheimer's disease based on the fusion of donepezil and melatonin.
China Pharmaceutical University
Design, Synthesis, and Evaluation of Donepezil-Like Compounds as AChE and BACE-1 Inhibitors.
Universit£
Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.
Tu Dortmund University
Bioactive Constituents of Glycyrrhiza uralensis (Licorice): Discovery of the Effective Components of a Traditional Herbal Medicine.
Peking University
Acetylcholinesterase and carbonic anhydrase inhibitory properties of novel urea and sulfamide derivatives incorporating dopaminergic 2-aminotetralin scaffolds.
Erzurum Technical University
Discovery of Highly Selective and Nanomolar Carbamate-Based Butyrylcholinesterase Inhibitors by Rational Investigation into Their Inhibition Mode.
Universit£T W£Rzburg
Amyloid cascade in Alzheimer's disease: Recent advances in medicinal chemistry.
University Of Waterloo
Application of PEG-400 as a green biodegradable polymeric medium for the catalyst-free synthesis of spiro-dihydropyridines and their use as acetyl and butyrylcholinesterase inhibitors.
Persian Gulf University
Design, synthesis and biological evaluation of novel donepezil-coumarin hybrids as multi-target agents for the treatment of Alzheimer's disease.
China Pharmaceutical University
Avertoxins A-D, Prenyl Asteltoxin Derivatives from Aspergillus versicolor Y10, an Endophytic Fungus of Huperzia serrata.
Fujian Normal University
Cardanol-derived AChE inhibitors: Towards the development of dual binding derivatives for Alzheimer's disease.
University Of Bras£Lia
Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.
China Pharmaceutical University
Tacrine-Trolox Hybrids: A Novel Class of Centrally Active, Nonhepatotoxic Multi-Target-Directed Ligands Exerting Anticholinesterase and Antioxidant Activities with Low In Vivo Toxicity.
University Hospital Hradec Kralove
A computational view on the significance of E-ring in binding of (+)-arisugacin A to acetylcholinesterase.
Alchemical Research
New multifunctional melatonin-derived benzylpyridinium bromides with potent cholinergic, antioxidant, and neuroprotective properties as innovative drugs for Alzheimer's disease.
1St Affiliated Hospital Of Guangxi Medical University
Difluoromethyl ketones: Potent inhibitors of wild type and carbamate-insensitive G119S mutant Anopheles gambiae acetylcholinesterase.
Virginia Tech
Synthesis, biological evaluation and molecular modeling of new tetrahydroacridine derivatives as potential multifunctional agents for the treatment of Alzheimer's disease.
Jagiellonian University Medical College
Carbamoyl Triazoles, Known Serine Protease Inhibitors, Are a Potent New Class of Antimalarials.
Glaxosmithkline
Synthesis of novel triazoles and a tetrazole of escitalopram as cholinesterase inhibitors.
University Of The Punjab
Synthesis, biological profiling and mechanistic studies of 4-aminoquinoline-based heterodimeric compounds with dual trypanocidal-antiplasmodial activity.
Universitat De Barcelona
In vitro evaluation and in silico screening of synthetic acetylcholinesterase inhibitors bearing functionalized piperidine pharmacophores.
Visva-Bharati (A Central University)
Synthesis and in vitro kinetic evaluation of N-thiazolylacetamido monoquaternary pyridinium oximes as reactivators of sarin, O-ethylsarin and VX inhibited human acetylcholinesterase (hAChE).
Defence Research & Development Establishment (Drde)
From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.
University Of Bologna
Design, synthesis and evaluation of novel tacrine-(ß-carboline) hybrids as multifunctional agents for the treatment of Alzheimer's disease.
China Pharmaceutical University
Design, synthesis and pharmacological evaluation of chalcone derivatives as acetylcholinesterase inhibitors.
Hu'Nan University
Discovery of potent carbonic anhydrase and acetylcholine esterase inhibitors: novel sulfamoylcarbamates and sulfamides derived from acetophenones.
Agriibrahim£E£En University
Structure-Based Design and Optimization of Multitarget-Directed 2H-Chromen-2-one Derivatives as Potent Inhibitors of Monoamine Oxidase B and Cholinesterases.
Universit£
Isolation of cholinesterase andß-secretase 1 inhibiting compounds from Lycopodiella cernua.
Catholic University Of Daegu
Mitigation of Acetylcholine Esterase Activity in the 1,7-Diazacarbazole Series of Inhibitors of Checkpoint Kinase 1.
Argenta Discovery
Polycyclic Polyprenylated Acylphloroglucinol Congeners Possessing Diverse Structures from Hypericum henryi.
Chinese Academy Of Sciences
Design, synthesis and evaluation of scutellarein-O-alkylamines as multifunctional agents for the treatment of Alzheimer's disease.
Sichuan University
Multi-target tacrine-coumarin hybrids: cholinesterase and monoamine oxidase B inhibition properties against Alzheimer's disease.
China Pharmaceutical University
Novel multitarget-directed ligands (MTDLs) with acetylcholinesterase (AChE) inhibitory and serotonergic subtype 4 receptor (5-HT4R) agonist activities as potential agents against Alzheimer's disease: the design of donecopride.
Cermn
Recent advances of chroman-4-one derivatives: synthetic approaches and bioactivities.
Mazandaran University Of Medical Sciences
Development of multifunctional, heterodimeric isoindoline-1,3-dione derivatives as cholinesterase andß-amyloid aggregation inhibitors with neuroprotective properties.
Jagiellonian University Medical College
Multifunctional tacrine-trolox hybrids for the treatment of Alzheimer's disease with cholinergic, antioxidant, neuroprotective and hepatoprotective properties.
China Pharmaceutical University
N-Methyl-N-((1-methyl-5-(3-(1-(2-methylbenzyl)piperidin-4-yl)propoxy)-1H-indol-2-yl)methyl)prop-2-yn-1-amine, a new cholinesterase and monoamine oxidase dual inhibitor.
Laboratorio De Quimica Medica (Iqog, Csic)
Synthesis and biological evaluation of open-chain analogs of cyclic peptides as inhibitors of cellular Shp2 activity.
Hebei University Of Science & Technology
Design, synthesis and evaluation of novel 5,6,7-trimethoxyflavone-6-chlorotacrine hybrids as potential multifunctional agents for the treatment of Alzheimer's disease.
Wenzhou Medical University
Isoindoline-1,3-dione derivatives targeting cholinesterases: design, synthesis and biological evaluation of potential anti-Alzheimer's agents.
Jagiellonian University Medical College
3-Oxoisoxazole-2(3H)-carboxamides and isoxazol-3-yl carbamates: Resistance-breaking acetylcholinesterase inhibitors targeting the malaria mosquito, Anopheles gambiae.
Virginia Tech
Synthesis and biological evaluation of novel tacrine derivatives and tacrine-coumarin hybrids as cholinesterase inhibitors.
P. J. Safarik University
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aß aggregation, andß-secretase.
Central China Normal University
Amine substitution of quinazolinones leads to selective nanomolar AChE inhibitors with 'inverted' binding mode.
Universit£T Regensburg
Tetrahydrobenzo[h][1,6]naphthyridine-6-chlorotacrine hybrids as a new family of anti-Alzheimer agents targetingß-amyloid, tau, and cholinesterase pathologies.
Universitat De Barcelona
Synthesis and characterization of novel 1,2-oxazine-based small molecules that targets acetylcholinesterase.
N.D. Zelinsky Institute Of Organic Chemistry
Biased and unbiased strategies to identify biologically active small molecules.
Institut De Chimie Des Substances Naturelles
Sulfonamides as multifunctional agents for Alzheimer's disease.
University Of Massachusetts Boston
Anithiactins A-C, modified 2-phenylthiazoles from a mudflat-derived Streptomyces sp.
Seoul National University
Synthesis and antiprotozoal activity of oligomethylene- and p-phenylene-bis(methylene)-linked bis(+)-huprines.
TBA
Protective effects of aloe-emodin on scopolamine-induced memory impairment in mice and H2O2-induced cytotoxicity in PC12 cells.
TBA
New efficient imidazolium aldoxime reactivators for nerve agent-inhibited acetylcholinesterase.
Institute Of Pharmacology And Toxicology
Multitarget drug design strategy: quinone-tacrine hybrids designed to block amyloid-ß aggregation and to exert anticholinesterase and antioxidant effects.
Alma Mater Studiorum-University Of Bologna
Discovery, biological evaluation, and crystal structure of a novel nanomolar selective butyrylcholinesterase inhibitor.
University Of Ljubljana
Biotransformation of huperzine A by a fungal endophyte of Huperzia serrata furnished sesquiterpenoid-alkaloid hybrids.
Zhejiang University
Assessment of antidotal efficacy of cholinesterase reactivators against paraoxon: In vitro reactivation kinetics and physicochemical properties.
Pt. Ravishankar Shukla University
Design, synthesis and biological evaluation of novel 6H-benzo[c]chromen-6-one, and 7,8,9,10-tetrahydro-benzo[c]chromen-6-one derivatives as potential cholinesterase inhibitors.
Eastern Mediterranean University
Shogaol-huprine hybrids: dual antioxidant and anticholinesterase agents withß-amyloid and tau anti-aggregating properties.
Universitat De Barcelona
Synthesis ofa,ß-unsaturated carbonyl based compounds as acetylcholinesterase and butyrylcholinesterase inhibitors: characterization, molecular modeling, QSAR studies and effect against amyloidß-induced cytotoxicity.
Universiti Kebangsaan Malaysia
New melatonin-N,N-dibenzyl(N-methyl)amine hybrids: potent neurogenic agents with antioxidant, cholinergic, and neuroprotective properties as innovative drugs for Alzheimer's disease.
Instituto De Qu£Mica M£Dica
Design, synthesis and biological evaluation of benzylisoquinoline derivatives as multifunctional agents against Alzheimer's disease.
China Pharmaceutical University
Synthesis and in vitro evaluation of bis-quaternary 2-(hydroxyimino)-N-(pyridin-3-yl)acetamide derivatives as reactivators against sarin and VX inhibited human acetylcholinesterase (hAChE).
Defence Research & Development Establishment (Drde)
Design, synthesis, and characterization of novel, nonquaternary reactivators of GF-inhibited human acetylcholinesterase.
Southwest Research Institute
Alkaloids from the roots of Stichoneuron caudatum and their acetylcholinesterase inhibitory activities.
University Of Wollongong
Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents.
Universitat De Barcelona
Oxidative stress in Alzheimer's disease: are we connecting the dots?
University Of Bologna
Design, synthesis and biological evaluation of novel tetrahydroacridine pyridine- aldoxime and -amidoxime hybrids as efficient uncharged reactivators of nerve agent-inhibited human acetylcholinesterase.
University Of Strasburg
Design, synthesis, acetylcholinesterase inhibition and larvicidal activity of girgensohnine analogs on Aedes aegypti, vector of dengue fever.
Universidad Industrial De Santander
Fluorinated benzophenone derivatives: balanced multipotent agents for Alzheimer's disease.
University Of Bologna
Quinolone-benzylpiperidine derivatives as novel acetylcholinesterase inhibitor and antioxidant hybrids for Alzheimer disease.
Universit£
Multifunctional cholinesterase and amyloid Beta fibrillization modulators. Synthesis and biological investigation.
University Of Siena
Preparation, in vitro evaluation and molecular modelling of pyridinium-quinolinium/isoquinolinium non-symmetrical bisquaternary cholinesterase inhibitors.
Charles University In Prague
Novel tacrine-ebselen hybrids with improved cholinesterase inhibitory, hydrogen peroxide and peroxynitrite scavenging activity.
Sun Yat-Sen University
Synthesis and discovery of novel piperidone-grafted mono- and bis-spirooxindole-hexahydropyrrolizines as potent cholinesterase inhibitors.
Universiti Sains Malaysia
Structural analogs of huperzine A improve survival in guinea pigs exposed to soman.
University Of Illinois At Chicago
Modulation of esterified drug metabolism by tanshinones from Salvia miltiorrhiza ("Danshen").
St. Jude Children'S Research Hospital
Design, synthesis and evaluation of novel heterodimers of donepezil and huperzine fragments as acetylcholinesterase inhibitors.
The Hong Kong University Of Science And Technology
Synthesis, molecular modeling and evaluation of novel N'-2-(4-benzylpiperidin-/piperazin-1-yl)acylhydrazone derivatives as dual inhibitors for cholinesterases and Aß aggregation.
Baskent University
Additional acetyl cholinesterase inhibitory property of diaryl pyrazoline derivatives.
Birla Institute Of Technology
Design, synthesis and biological evaluation of coumarin alkylamines as potent and selective dual binding site inhibitors of acetylcholinesterase.
Universit£
Structure-activity relationships of methoctramine-related polyamines as muscarinic antagonist: effect of replacing the inner polymethylene chain with cyclic moieties.
Universit£
Modulation of binding strength in several classes of active site inhibitors of acetylcholinesterase studied by comparative binding energy analysis.
Universitat De Barcelona
Structure-activity relationships of methoctramine-related polyamines as muscular nicotinic receptor noncompetitive antagonists. 3. Effect of inserting the tetraamine backbone into a macrocyclic structure.
University Of Bologna
Hexahydrochromeno[4,3-b]pyrrole derivatives as acetylcholinesterase inhibitors.
University Of Bologna
3D-QSAR studies on natural acetylcholinesterase inhibitors of Sarcococca saligna by comparative molecular field analysis (CoMFA).
University Of Innsbruck
Receptor-dependent (RD) 3D-QSAR approach of a series of benzylpiperidine inhibitors of human acetylcholinesterase (HuAChE).
Universidade Federal Do Rio De Janeiro (Ufrj)
Three-dimensional quantitative structure-activity relationships from molecular similarity matrices and genetic neural networks. 2. Applications.
Harvard University
A comparative molecular field analysis study of N-benzylpiperidines as acetylcholinesterase inhibitors.
University Of Missouri St. Louis
Synthesis, biological assessment, and molecular modeling of racemic 7-aryl-9,10,11,12-tetrahydro-7H-benzo[7,8]chromeno[2,3-b]quinolin-8-amines as potential drugs for the treatment of Alzheimer's disease.
Universit£
Phenyltetrahydroisoquinoline-pyridinaldoxime conjugates as efficient uncharged reactivators for the dephosphylation of inhibited human acetylcholinesterase.
Universit£
Exploration of natural compounds as sources of new bifunctional scaffolds targeting cholinesterases and beta amyloid aggregation: the case of chelerythrine.
Abo Akademi University
Metaproterenol, isoproterenol, and their bisdimethylcarbamate derivatives as human cholinesterase inhibitors.
Institute For Medical Research And Occupational Health
2-Arylbenzofuran-based molecules as multipotent Alzheimer's disease modifying agents.
University Of Bologna
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aß aggregation, andß-secretase.
Central China Normal University
O-Hydroxyl- or o-amino benzylamine-tacrine hybrids: multifunctional biometals chelators, antioxidants, and inhibitors of cholinesterase activity and amyloid-ß aggregation.
Sun Yat-Sen University
Pyridonepezils, new dual AChE inhibitors as potential drugs for the treatment of Alzheimer's disease: synthesis, biological assessment, and molecular modeling.
Instituto De Qu£Mica Org£Nica General (Csic)
Geranylphenazinediol, an acetylcholinesterase inhibitor produced by a Streptomyces species.
Kieler Wirkstoff-Zentrum (Kiwiz) At The Helmholtz-Zenrum F�R Ozeanforschung Geomar
Synthesis, design and biological evaluation of novel highly potent tacrine congeners for the treatment of Alzheimer's disease.
P. J. Safarik University
Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.
University Of Waterloo
Multipotent MAO and cholinesterase inhibitors for the treatment of Alzheimer's disease: synthesis, pharmacological analysis and molecular modeling of heterocyclic substituted alkyl and cycloalkyl propargyl amine.
Laboratorio De Radicales Libres Y Qu�Mica Computacional (Iqog, Csic)
Prospective acetylcholinesterase inhibitory activity of indole and its analogs.
Naresuan University
New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, andß-amyloid-reducing properties.
Instituto De Qu£Mica M£Dica
Cholinestrase inhibitory effects of geranylated flavonoids from Paulownia tomentosa fruits.
Graduate School Of Gyeongsang National University
Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.
Universitat De Barcelona
Discovery of {1-[4-(2-{hexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl}-1H-benzimidazol-1-yl)piperidin-1-yl]cyclooctyl}methanol, systemically potent novel non-peptide agonist of nociceptin/orphanin FQ receptor as analgesic for the treatment of neuropathic pain: design, synthesis, and structure-activity rela
Pfizer
Preparation, in vitro screening and molecular modelling of symmetrical 4-tert-butylpyridinium cholinesterase inhibitors--analogues of SAD-128.
University Of Defence
Mono-oxime bisquaternary acetylcholinesterase reactivators with prop-1,3-diyl linkage-Preparation, in vitro screening and molecular docking.
University Of Defence
Substituted spiro [2.3'] oxindolespiro [3.2¿]-5,6-dimethoxy-indane-1¿-one-pyrrolidine analogue as inhibitors of acetylcholinesterase.
Universiti Sains Malaysia
Discovery of N-{1-[3-(3-oxo-2,3-dihydrobenzo[1,4]oxazin-4-yl)propyl]piperidin-4-yl}-2-phenylacetamide (Lu AE51090): an allosteric muscarinic M1 receptor agonist with unprecedented selectivity and procognitive potential.
H. Lundbeck
Long-acting anticholinesterases for myasthenia gravis: synthesis and activities of quaternary phenylcarbamates of neostigmine, pyridostigmine and physostigmine.
National Institute On Aging
Synthesis, inhibitory activity of cholinesterases, and neuroprotective profile of novel 1,8-naphthyridine derivatives.
Universidad Autonoma De Madrid
Probing Torpedo californica acetylcholinesterase catalytic gorge with two novel bis-functional galanthamine derivatives.
Istituto Di Cristallografia
Structural aspects of flavonoids as inhibitors of human butyrylcholinesterase.
Institute For Medical Research And Occupational Health
Synthesis and structure-activity relationship of Huprine derivatives as human acetylcholinesterase inhibitors.
Cobra
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 4. Further investigation on the inner spacer.
University Of Bologna
New tacrine-dihydropyridine hybrids that inhibit acetylcholinesterase, calcium entry, and exhibit neuroprotection properties.
Laboratorio De Radicales Libres (Iqog, Csic)
Taspine: bioactivity-guided isolation and molecular ligand-target insight of a potent acetylcholinesterase inhibitor from Magnolia x soulangiana.
Leopold-Franzens-Universit£T
Coumarins isolated from Angelica gigas inhibit acetylcholinesterase: structure-activity relationships.
Seoul National University
Novel donepezil-based inhibitors of acetyl- and butyrylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
Laboratori De Qu�Mica Farmac�Utica (Unitat Associada Al Csic)
Exploiting protein fluctuations at the active-site gorge of human cholinesterases: further optimization of the design strategy to develop extremely potent inhibitors.
Universit£
Lead identification of acetylcholinesterase inhibitors-histamine H3 receptor antagonists from molecular modeling.
Johnson & Johnson Pharmaceutical Research And Development
Bis-(-)-nor-meptazinols as novel nanomolar cholinesterase inhibitors with high inhibitory potency on amyloid-beta aggregation.
Fudan University
Synthesis and biological evaluation of NO-donor-tacrine hybrids as hepatoprotective anti-Alzheimer drug candidates.
TBA
Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds.
University Of Bologna
Multi-target-directed ligands to combat neurodegenerative diseases.
University Of Bologna
4-Aminopyridine derivatives with anticholinesterase and antiamnesic activity.
Sapienza University Of Rome
Benzylphenethylamine alkaloids from Hosta plantaginea with inhibitory activity against tobacco mosaic virus and acetylcholinesterase.
Chinese Academy Of Sciences
First gallamine-tacrine hybrid: design and characterization at cholinesterases and the M2 muscarinic receptor.
University Of Bonn
Synthesis and screening for acetylcholinesterase inhibitor activity of some novel 2-butyl-1,3-diaza-spiro[4,4]non-1-en-4-ones: derivatives of irbesartan key intermediate.
University Of Mysore
Novel class of quinone-bearing polyamines as multi-target-directed ligands to combat Alzheimer's disease.
University Of Bologna
Binding of 13-amidohuprines to acetylcholinesterase: exploring the ligand-induced conformational change of the gly117-gly118 peptide bond in the oxyanion hole.
Universitat De Barcelona
Isoquinoline derivatives as potential acetylcholinesterase inhibitors.
Naresuan University
Novel anticholinesterases based on the molecular skeletons of furobenzofuran and methanobenzodioxepine.
National Institute On Aging
Further studies on the interaction of the 5-hydroxytryptamine3 (5-HT3) receptor with arylpiperazine ligands. development of a new 5-HT3 receptor ligand showing potent acetylcholinesterase inhibitory properties.
Universit£
Propidium-based polyamine ligands as potent inhibitors of acetylcholinesterase and acetylcholinesterase-induced amyloid-beta aggregation.
University Of Bologna
A docking score function for estimating ligand-protein interactions: application to acetylcholinesterase inhibition.
University Of Kansas
Specific targeting of acetylcholinesterase and butyrylcholinesterase recognition sites. Rational design of novel, selective, and highly potent cholinesterase inhibitors.
Universit£
Synthesis, in vitro pharmacology, and molecular modeling of syn-huprines as acetylcholinesterase inhibitors.
Universitat De Barcelona
Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors.
Universit£
New tacrine-huperzine A hybrids (huprines): highly potent tight-binding acetylcholinesterase inhibitors of interest for the treatment of Alzheimer's disease.
Universitat De Barcelona
Mixture-based synthetic combinatorial libraries.
Torrey Pines Institute For Molecular Studies
Acetylcholinesterase noncovalent inhibitors based on a polyamine backbone for potential use against Alzheimer's disease.
University Of Bologna
Structure-based alignment and comparative molecular field analysis of acetylcholinesterase inhibitors.
University Of North Carolina
Design and synthesis of 1-heteroaryl-3-(1-benzyl-4-piperidinyl)propan-1-one derivatives as potent, selective acetylcholinesterase inhibitors.
Pfizer
Synthesis of 2-imidazolidinylidenepropanedinitrile derivatives as stimulators of gastrointestinal motility.
Kyowa Hakko Kogyo
Syntheses, resolution, and structure-activity relationships of potent acetylcholinesterase inhibitors: 8-carbaphysostigmine analogues.
Pfizer
Synthesis and cholinergic properties of bis[[(dimethylamino)methyl]furanyl] analogues of ranitidine.
University Of South Carolina
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 4. Effect of various side-chain substituents on therapeutic activity against anticholinesterase intoxication.
Sri International
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 2. Preparation and in vitro and in vivo evaluation of 1-(alkoxymethyl)-2-[(hydroxyimino)methyl]-3-methylimida zolium halides for reactivation of organophosphorus-inhibited acetylcholinesterases.
Sri International
Nonquaternary cholinesterase reactivators. 4. Dialkylaminoalkyl thioesters of alpha-keto thiohydroximic acids as reactivators of ethyl methylphosphonyl- and 1,2,2-trimethylpropyl methylphosphonyl-acetylcholinesterase in vitro.
TBA
Anionic cyclophanes as potential reversal agents of muscle relaxants by chemical chelation.
Organon Laboratories
Novel piperidinium and pyridinium agents as water-soluble acetylcholinesterase inhibitors for the reversal of neuromuscular blockade.
Organon Laboratories
Quaternary salts of E2020 analogues as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
Organon Laboratories
Synthesis and acetylcholinesterase inhibitory activity of fluorinated analogues of huperzine A
TBA
Amidine-oximes: reactivators for organophosphate exposure.
Human Biomolecular Research Institute
Nonquaternary reactivators for organophosphate-inhibited cholinesterases.
Human Biomolecular Research Institute
A review on coumarins as acetylcholinesterase inhibitors for Alzheimer's disease.
Punjabi University
Synthesis of monomeric derivatives to probe memoquin's bivalent interactions.
University Of Bologna
Synthesis, biological evaluation, and molecular modeling of donepezil and N-[(5-(benzyloxy)-1-methyl-1H-indol-2-yl)methyl]-N-methylprop-2-yn-1-amine hybrids as new multipotent cholinesterase/monoamine oxidase inhibitors for the treatment of Alzheimer's disease.
Universitat Aut£Noma De Barcelona
Searching for the Multi-Target-Directed Ligands against Alzheimer's disease: discovery of quinoxaline-based hybrid compounds with AChE, H3R and BACE 1 inhibitory activities.
Zhejiang University
Synthesis and testing of trifluoromethyl-containing phosphonate-peptide conjugates as inhibitors of serine hydrolases.
Moscow State University
Synthesis and biological assessment of diversely substituted furo[2,3-b]quinolin-4-amine and pyrrolo[2,3-b]quinolin-4-amine derivatives, as novel tacrine analogues.
University Of Lisbon
Investigation of the pyrazinones as PDE5 inhibitors: evaluation of regioisomeric projections into the solvent region.
Pfizer
Selective cholinesterase inhibition by lanostane triterpenes from fruiting bodies of Ganoderma lucidum.
Chungnam National University
Synthesis and in vitro evaluation of 7-methoxy-N-(pent-4-enyl)-1,2,3,4-tetrahydroacridin-9-amine-new tacrine derivate with cholinergic properties.
Charles University In Prague
Exploiting the lipoic acid structure in the search for novel multitarget ligands against Alzheimer's disease.
University Of Bologna
Benzofurans from Styrax agrestis as acetylcholinesterase inhibitors: structure-activity relationships and molecular modeling studies.
Guangzhou University Of Chinese Medicine
Development of 2-substituted-N-(naphth-1-ylmethyl) and N-benzhydrylpyrimidin-4-amines as dual cholinesterase and Aß-aggregation inhibitors: Synthesis and biological evaluation.
University Of Waterloo
Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.
Institut F£R Molekulare Physiologie
Requirements for mammalian carboxylesterase inhibition by substituted ethane-1,2-diones.
St. Jude Children'S Research Hospital
Synthesis, biological activity and HPLC validation of 1,2,3,4-tetrahydroacridine derivatives as acetylcholinesterase inhibitors.
Medical University
Quinolizidinyl derivatives of bi- and tricyclic systems as potent inhibitors of acetyl- and butyrylcholinesterase with potential in Alzheimer's disease.
Universit£
New potent human acetylcholinesterase inhibitors in the tetracyclic triterpene series with inhibitory potency on amyloid β aggregation.
Cnrs
Synthesis and biological evaluation of novel gamma-carboline analogues of Dimebon as potent 5-HT6 receptor antagonists.
Chemical Diversity Research Institute
Novel carbamate cholinesterase inhibitors that release biologically active amines following enzyme inhibition.
Sention
Benzophenone-based derivatives: a novel series of potent and selective dual inhibitors of acetylcholinesterase and acetylcholinesterase-induced beta-amyloid aggregation.
University Of Bologna
Homodimeric bis-quaternary heterocyclic ammonium salts as potent acetyl- and butyrylcholinesterase inhibitors: a systematic investigation of the influence of linker and cationic heads over affinity and selectivity.
Universidad De Granada
Multitargeted drugs discovery: balancing anti-amyloid and anticholinesterase capacity in a single chemical entity.
Department Of Pharmaceutical Sciences-Alma Mater Studiorum-Bologna University
(+)-Arisugacin A--computational evidence of a dual binding site covalent inhibitor of acetylcholinesterase.
Alchemical Research
Design, synthesis and structure-activity relationship (SAR) studies of 2,4-disubstituted pyrimidine derivatives: dual activity as cholinesterase and A β-aggregation inhibitors.
University Of Waterloo
Preparation, in vitro screening and molecular modelling of symmetrical bis-quinolinium cholinesterase inhibitors--implications for early myasthenia gravis treatment.
Charles University
Preparation and in vitro screening of symmetrical bis-isoquinolinium cholinesterase inhibitors bearing various connecting linkage--implications for early Myasthenia gravis treatment.
University Of Defence
Triterpenoidal alkaloids from Buxus natalensis and their acetylcholinesterase inhibitory activity.
The University Of Winnipeg
Structure-activity relationships of substituted 1-pyridyl-2-phenyl-1,2-ethanediones: potent, selective carboxylesterase inhibitors.
St. Jude Children'S Research Hospital
Synthesis, characterization, oxidative degradation, antibacterial activity and acetylcholinesterase/butyrylcholinesterase inhibitory effects of some new phosphorus(V) hydrazides.
Tarbiat Modares University
Synthesis and in vitro evaluation of N-alkyl-7-methoxytacrine hydrochlorides as potential cholinesterase inhibitors in Alzheimer disease.
Charles University
Novel carbamates as orally active acetylcholinesterase inhibitors found to improve scopolamine-induced cognition impairment: pharmacophore-based virtual screening, synthesis, and pharmacology.
Central Drug Research Institute
Structure-activity studies on acetylcholinesterase inhibition in the lycorine series of Amaryllidaceae alkaloids.
Mcmaster University
Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.
University Of Bologna
Novel tacrine-8-hydroxyquinoline hybrids as multifunctional agents for the treatment of Alzheimer's disease, with neuroprotective, cholinergic, antioxidant, and copper-complexing properties.
Instituto De Quimica Medica
Prediction of acetylcholinesterase inhibitors and characterization of correlative molecular descriptors by machine learning methods.
Sichuan University
Molecular modelling, synthesis and acetylcholinesterase inhibition of ethyl 5-amino-2-methyl-6,7,8,9-tetrahydrobenzo[b][1,8]naphthyridine-3-carboxylate.
Laboratorio De Radicales Libres Y QuÍMica Computacional (Iqog, Csic)
Preparation and in vitro screening of symmetrical bispyridinium cholinesterase inhibitors bearing different connecting linkage-initial study for Myasthenia gravis implications.
Military Health Sciences
Neuroprotective and cholinergic properties of multifunctional glutamic acid derivatives for the treatment of Alzheimer's disease.
Instituto De Quimica Medica (Csic)
Synthesis and kinetic analysis of some phosphonate analogs of cyclophostin as inhibitors of human acetylcholinesterase.
University Of Missouri St. Louis
Differential binding of phenothiazine urea derivatives to wild-type human cholinesterases and butyrylcholinesterase mutants.
Dalhousie University
Targeting Alzheimer's disease: Novel indanone hybrids bearing a pharmacophoric fragment of AP2238.
University Of Bologna
Rational design and synthesis of highly potent anti-acetylcholinesterase activity huperzine A derivatives.
The Chinese Academy Of Sciences
Toward a rational design of multitarget-directed antioxidants: merging memoquin and lipoic acid molecular frameworks.
University Of Bologna
Active site directed docking studies: synthesis and pharmacological evaluation of cis-2,6-dimethyl piperidine sulfonamides as inhibitors of acetylcholinesterase.
University Of Mysore
Pyrrolidinoindoline alkaloids from Selaginella moellendorfii.
Chinese Academy Of Sciences
Structure-activity relationships of memoquin: Influence of the chain chirality in the multi-target mechanism of action.
Alma Mater Studiorum-Bologna University
Antioxidant and anticholinesterase activity evaluation of ent-kaurane diterpenoids from Sideritis arguta.
Istanbul University
Imino 1,2,3,4-tetrahydrocyclopent[b]indole carbamates as dual inhibitors of acetylcholinesterase and monoamine oxidase
TBA
Synthesis and structure-activity relationships of new acetylcholinesterase inhibitors: Morpholinoalkylcarbamoyloxyeseroline derivatives
TBA
The synthesis and in vitro acetylcholinesterase and butyrylcholinesterase inhibitory activity of tacrine (Cognex®) derivaties
TBA
Total synthesis of an optically active 8-carba-physostigmine analog: a potent acetylcholinesterase inhibitor
TBA
Isosorbide-2-carbamate esters: potent and selective butyrylcholinesterase inhibitors.
Trinity College
Tacrine based human cholinesterase inhibitors: synthesis of peptidic-tethered derivatives and their effect on potency and selectivity.
European Research Centre For Drug Discovery And Development (Natsyndrugs)
Synthesis and elastase-inhibiting activity of 2-pyridinyl-isothiazol-3(2H)-one 1,1-dioxides.
University Of Leipzig
Bioactive 5alpha-pregnane-type steroidal alkaloids from Sarcococca hookeriana.
Bielefeld University
Solid-phase synthesis and biological evaluation of a parallel library of 2,3-dihydro-1,5-benzothiazepines.
Quaid-I-Azam University
Inhibition of acetylcholinesterase, beta-amyloid aggregation, and NMDA receptors in Alzheimer's disease: a promising direction for the multi-target-directed ligands gold rush.
University Of Bologna
Design, synthesis and evaluation of isaindigotone derivatives as acetylcholinesterase and butyrylcholinesterase inhibitors.
Sun Yat-Sen University
Benzofuran-based hybrid compounds for the inhibition of cholinesterase activity, beta amyloid aggregation, and abeta neurotoxicity.
University Of Bologna
Design, synthesis, and evaluation of benzophenone derivatives as novel acetylcholinesterase inhibitors.
University Of Bologna
The application of HPLC with on-line coupled UV/MS-biochemical detection for isolation of an acetylcholinesterase inhibitor from narcissus 'Sir Winston Churchill'.
Leiden University
Multi-target-directed drug design strategy: from a dual binding site acetylcholinesterase inhibitor to a trifunctional compound against Alzheimer's disease.
Bologna University
Synthesis and structure-activity relationship for a novel class of potent and selective carbamate-based inhibitors of hormone selective lipase with acute in vivo antilipolytic effects.
Novo Nordisk
Extensive SAR and computational studies of 3-{4-[(benzylmethylamino)methyl]phenyl}-6,7-dimethoxy-2H-2-chromenone (AP2238) derivatives.
University Of Bologna
Analysis of the inhibition of mammalian carboxylesterases by novel fluorobenzoins and fluorobenzils.
St. Jude Children'S Research Hospital
Novel multipotent tacrine-dihydropyridine hybrids with improved acetylcholinesterase inhibitory and neuroprotective activities as potential drugs for the treatment of Alzheimer's disease.
Laboratorio De Radicales Libres (Iqog, Csic)
Cholinesterase inhibitors: SAR and enzyme inhibitory activity of 3-[omega-(benzylmethylamino)alkoxy]xanthen-9-ones.
University Of Bologna
6-Hydroxy- and 6-methoxy-beta-carbolines as acetyl- and butyrylcholinesterase inhibitors.
Friedrich-Schiller-UniversitäT Jena
Novel selective inhibitors of neutral endopeptidase for the treatment of female sexual arousal disorder. Synthesis and activity of functionalized glutaramides.
Pfizer
Synthesis and efficacy of 1-[bis(4-fluorophenyl)-methyl]piperazine derivatives for acetylcholinesterase inhibition, as a stimulant of central cholinergic neurotransmission in Alzheimer's disease.
University Of Mysore
Inhibition of carboxylesterases by benzil (diphenylethane-1,2-dione) and heterocyclic analogues is dependent upon the aromaticity of the ring and the flexibility of the dione moiety.
St. Jude Children'S Research Hospital
Synthesis of tricyclic analogs of stephaoxocanidine and their evaluation as acetylcholinesterase inhibitors.
Universidad Nacional De Rosario
Anchor-GRIND: filling the gap between standard 3D QSAR and the GRid-INdependent descriptors.
Imim/Universitat Pompeu Fabra
A rate determining step change in the pre-steady state of acetylcholinesterase inhibitions by 1,n-alkane-di-N-butylcarbamates.
National Chung-Hsing University
Isoterreulactone A, a novel meroterpenoid with anti-acetylcholinesterase activity produced by Aspergillus terreus.
Korea Research Institute Of Bioscience And Biotechnology
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 3. Effect of replacing the inner polymethylene chain with cyclic moieties.
University Of Bologna
Acetylcholinesterase inhibitory activity of scopolin and scopoletin discovered by virtual screening of natural products.
Leopold-Franzens University Of Innsbruck
Synthesis and structure-activity relationship for a novel class of potent and selective carbamoyl-triazole based inhibitors of hormone sensitive lipase.
Novo Nordisk
Design and synthesis of pyrrolidine-5,5'-trans-lactams (5-oxo-hexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 4. Antiviral activity and plasma stability.
Glaxosmithkline
Structure-activity relationships of acetylcholinesterase noncovalent inhibitors based on a polyamine backbone. 2. Role of the substituents on the phenyl ring and nitrogen atoms of caproctamine.
University Of Bologna
Oxyaniliniums as acetylcholinesterase inhibitors for the reversal of neuromuscular block.
Organon Laboratories
Design and synthesis of pyrrolidine-5,5-trans-lactams (5-oxohexahydropyrrolo[3,2-b]pyrroles) as novel mechanism-based inhibitors of human cytomegalovirus protease. 2. Potency and chirality.
Glaxosmithkline
Synthesis and screening for antiacetylcholinesterase activity of (1-benzyl-4-oxopiperidin-3-ylidene)methylindoles and -pyrroles related to donepezil.
Università
Synthetic conversion of ACAT inhibitor to acetylcholinesterase inhibitor.
Kitasato University
Synthesis of novel phenserine-based-selective inhibitors of butyrylcholinesterase for Alzheimer's disease.
National Institute On Aging Intramural Research Program
Design and synthesis of monocyclic beta-lactams as mechanism-based inhibitors of human cytomegalovirus protease.
Glaxo Wellcome Research And Development
Synthesis and activity studies of N-[omega-N'-(adamant-1'-yl)aminoalkyl]- 2-(4'-dimethylaminophenyl)acetamides: in the search of selective inhibitors for the different molecular forms of acetylcholinesterase.
Istituto Di Strutturistica Chimica G. Giacomello
Synthesis and study of thiocarbonate derivatives of choline as potential inhibitors of acetylcholinesterase.
University Of North Texas
Total syntheses and anticholinesterase activities of (3aS)-N(8)-norphysostigmine, (3aS)-N(8)-norphenserine, their antipodal isomers, and other N(8)-substituted analogues.
National Institute On Aging
Identification of a 3-hydroxylated tacrine metabolite in rat and man: metabolic profiling implications and pharmacology.
Warner-Lambert
Novel benzisoxazole derivatives as potent and selective inhibitors of acetylcholinesterase.
Pfizer
5,7-dihydro-3-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-6H- pyrrolo[3,2-f]-1,2-benzisoxazol-6-one: a potent and centrally-selective inhibitor of acetylcholinesterase with an improved margin of safety.
Pfizer
Structure-activity relationships for reactivators of organophosphorus-inhibited acetylcholinesterase: quaternary salts of 2-[(hydroxyimino)methyl]imidazole.
TBA
Nonquaternary cholinesterase reactivators. 3. 3(5)-Substituted 1,2,4-oxadiazol-5(3)-aldoximes and 1,2,4-oxadiazole-5(3)-thiocarbohydroximates as reactivators of organophosphonate-inhibited eel and human acetylcholinesterase in vitro.
TBA
Carbamate ester derivatives as potential prodrugs of the presynaptic dopamine autoreceptor agonist (-)-3-(3-hydroxyphenyl)-N-propylpiperidine.
Astra Alab
Quaternary salts of 2-[(hydroxyimino)methyl]imidazole. 3. Synthesis and evaluation of (alkenyloxy)-, (alkynyloxy)-, and (aralkyloxy)methyl quaternarized 2-[(hydroxyimino)methyl]-1-alkylimidazolium halides as reactivators and therapy for soman intoxication.
Sri International
Alfred Burger award address. Bioactive alkaloids. 4. Results of recent investigations with colchicine and physostigmine.
Niddk
Conformational analyses and molecular-shape comparisons of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.
University Of Illinois
QSAR analyses of the substituted indanone and benzylpiperidine rings of a series of indanone-benzylpiperidine inhibitors of acetylcholinesterase.
University Of Illinois
Synthesis and cholinergic properties of N-aryl-2-[[[5-[(dimethylamino)methyl]-2-furanyl]methyl]thio]ethylamino analogs of ranitidine.
University Of South Carolina
A FLT3-inhibitory constituent from the rhizomes of Anemarrhena asphodeloides.
Gyeongsang National University
Differential activation of formyl peptide receptor signaling by peptide ligands.
Pohang University Of Science And Technology
Rofecoxib [Vioxx, MK-0966; 4-(4'-methylsulfonylphenyl)-3-phenyl-2-(5H)-furanone]: a potent and orally active cyclooxygenase-2 inhibitor. Pharmacological and biochemical profiles.
Merck Frosst Centre For Therapeutic Research
Cloning, expression and pharmacological characterization of rabbit adenosine A1 and A3 receptors.
Pfizer
Targeted polypharmacology: discovery of dual inhibitors of tyrosine and phosphoinositide kinases.
University Of California San Francisco
Discovery and SAR of 2-(1-propylpiperidin-4-yl)-1H-benzimidazole-4-carboxamide: A potent inhibitor of poly(ADP-ribose) polymerase (PARP) for the treatment of cancer.
Abbott Laboratories
Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity.
Astex
Potent inhibitors of HCV-NS3 protease derived from boronic acids.
Schering-Plough Research Institute
Cloning, expression, post-translational modifications and inhibition studies on the latest mammalian carbonic anhydrase isoform, CA XV.
University Of Tampere
Discovery, synthesis, and in vivo activity of a new class of pyrazoloquinazolines as selective inhibitors of aurora B kinase.
Astrazeneca
Structural Requirements for Eszopiclone and Zolpidem Binding to the gamma-Aminobutyric Acid Type-A (GABAA) Receptor Are Different.
University Of Wisconsin At Madison
Lead Optimization of 4-Acetylamino-2-(3,5-dimethylpyrazol-1-yl)-6-pyridylpyrimidines as A2A Adenosine Receptor Antagonists for the Treatment of Parkinson's Disease.
Neurocrine Bioscience
cis-4-(Piperazin-1-yl)-5,6,7a,8,9,10,11,11a-octahydrobenzofuro[2,3-h]quinazolin-2-amine (A-987306), A New Histamine H4R Antagonist that Blocks Pain Responses against Carrageenan-Induced Hyperalgesia.
Abbott Laboratories
The T790M mutation in EGFR kinase causes drug resistance by increasing the affinity for ATP.
Harvard Medical School
Indazole-Based Liver X Receptor (LXR) Modulators with Maintained Atherosclerotic Lesion Reduction Activity but Diminished Stimulation of Hepatic Triglyceride Synthesis
Wyeth Research
Identification of a new JNK inhibitor targeting the JNK-JIP interaction site.
Burnham Institute For Medical Research
Design and Synthesis of Orally Bioavailable Benzimidazoles as Raf Kinase Inhibitors.
Novartis
Design, synthesis, biological evaluation and pharmacokinetics of bis(hydroxyphenyl) substituted azoles, thiophenes, benzenes, and aza-benzenes as potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1).
Saarland University
Structure-based approach to the development of potent and selective inhibitors of dihydrofolate reductase from cryptosporidium.
University Of Connecticut At Storrs
Biochemically based design of cyclooxygenase-2 (COX-2) inhibitors: facile conversion of nonsteroidal antiinflammatory drugs to potent and highly selective COX-2 inhibitors.
Vanderbilt University School Of Medicine
4,5-dihydroxypyrimidine carboxamides and N-alkyl-5-hydroxypyrimidinone carboxamides are potent, selective HIV integrase inhibitors with good pharmacokinetic profiles in preclinical species.
Irbm-Mrl
Design and synthesis of bicyclic pyrimidinones as potent and orally bioavailable HIV-1 integrase inhibitors.
Irbm-Mrl
Structural insight into the pharmacophore pocket of human glutamate carboxypeptidase II.
Nci-Fcrdc