340 articles for thisTarget
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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
Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.
Bristol-Myers Squibb
Pregnane-10,2-carbolactones from a Hawaiian Marine Sponge in the Genus Myrmekioderma.
University Of Hawaii At Manoa
Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.
Tu Dortmund University
Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.
University Of Florida
Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors ofß-Secretase.
Amgen
Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain Aß Reduction in Rodents.
Bristol-Myers Squibb
Structure-Based Design of an Iminoheterocyclicß-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central Aß in Nonhuman Primates.
Merck Research Laboratories
Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors.
Birla Institute Of Technology
Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3ß Inhibitors.
Alma Mater Studiorum-University Of Bologna
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
Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.
Korea University Of Science And Technology
Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors.
Birla Institute Of Technology
1,4-Oxazineß-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.
Janssen Pharmaceutica
Macrocyclic prolinyl acyl guanidines as inhibitors ofß-secretase (BACE).
Bristol-Myers Squibb
Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors.
Kyoto Pharmaceutical University
From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.
University Of Bologna
Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.
The Walter And Eliza Hall Institute Of Medical Research
Peptidomimeticß-Secretase Inhibitors Comprising a Sequence of Amyloid-ß Peptide for Alzheimer's Disease.
Instituto De Biologia Experimental E Tecnol£Gica
Isolation of cholinesterase andß-secretase 1 inhibiting compounds from Lycopodiella cernua.
Catholic University Of Daegu
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.
Eli Lilly
4,6-Diarylaminothiazines as BACE1 Inhibitors and Their Use for the Reduction of Beta-Amyloid Production.
Temple University School Of Pharmacy
Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.
The Scripps Research Institute
Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.
Eurofarma Laboratorios
Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.
Fudan University
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.
Novartis Pharma
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.
Novartis Pharma
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.
Merck Research Laboratories
Novelß-amyloid aggregation inhibitors possessing a turn mimic.
Kobe Pharmaceutical University
An Orally Available BACE1 Inhibitor That Affords Robust CNS Aß Reduction without Cardiovascular Liabilities.
Amgen
Development of 2-aminooxazoline 3-azaxanthenes as orally efficaciousß-secretase inhibitors for the potential treatment of Alzheimer's disease.
Amgen
Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, Aß aggregation, andß-secretase.
Central China Normal University
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.
Novartis Institutes For Biomedical Research
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.
Purdue University
8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.
Array Biopharma
Lead optimization and modulation of hERG activity in a series of aminooxazoline xantheneß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Amgen
Inhibitors ofß-site amyloid precursor protein cleaving enzyme (BACE1): identification of (S)-7-(2-fluoropyridin-3-yl)-3-((3-methyloxetan-3-yl)ethynyl)-5'H-spiro[chromeno[2,3-b]pyridine-5,4'-oxazol]-2'-amine (AMG-8718).
Amgen
Dose-dependent inhibition of BACE-1 by the monoterpenoid 2,3,4,4-tetramethyl-5-methylenecyclopent-2-enone in cellular and mouse models of Alzheimer's disease.
University Of Coimbra
ß-Secretase (BACE1)-inhibiting C-methylrotenoids from Abronia nana suspension cultures.
Kyungpook National University
Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.
Genentech
Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents.
Universitat De Barcelona
4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies.
Peking University Health Science Center
?-Secretase Inhibitors for the Treatment of Alzheimer's Disease and Down's Syndrome.
Therachem Research Medilab (India)
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.
F. Hoffmann-La Roche
Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species.
Array Biopharma
Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors ofß-secretase (BACE1).
Tehran University Of Medical Sciences
Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.
Elan Pharmaceuticals
The discovery of novel potent trans-3,4-disubstituted pyrrolidine inhibitors of the human aspartic protease renin from in silico three-dimensional (3D) pharmacophore searches.
Novartis Pharma
Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design.
University Of Leeds
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.
Novartis Pharma
Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease.
Universidad Complutense
Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies.
Universit£
Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.
Astrazeneca
Self-organizing molecular field analysis on humanß-secretase nonpeptide inhibitors: 5, 5-disubstituted aminohydantoins.
Sichuan University
Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.
Universite£
Cyanobacterial peptides as a prototype for the design of potentß-secretase inhibitors and the development of selective chemical probes for other aspartic proteases.
University Of Florida
Acyl guanidine inhibitors ofß-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.
Bristol-Myers Squibb Research
New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain.
Astrazeneca
Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.
Merck Research Laboratories
Spirocyclic sulfamides asß-secretase 1 (BACE-1) inhibitors for the treatment of Alzheimer's disease: utilization of structure based drug design, WaterMap, and CNS penetration studies to identify centrally efficacious inhibitors.
Pfizer
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.
Purdue University
Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.
Amgen
Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides.
Astrazeneca
Discovery and optimization of a novel spiropyrrolidine inhibitor ofß-secretase (BACE1) through fragment-based drug design.
Pfizer
Design and synthesis of potent, orally efficacious hydroxyethylamine derivedß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.
Amgen
Design and preparation of a potent series of hydroxyethylamine containingß-secretase inhibitors that demonstrate robust reduction of centralß-amyloid.
Amgen
Conformational restriction approach toß-secretase (BACE1) inhibitors: effect of a cyclopropane ring to induce an alternative binding mode.
Shionogi
Structural modifications that alter the P-glycoprotein efflux properties of compounds.
Envoy Therapeutics
Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aß aggregation, andß-secretase.
Central China Normal University
Design and synthesis of potent hydroxyethylamine (HEA) BACE-1 inhibitors carrying prime side 4,5,6,7-tetrahydrobenzazole and 4,5,6,7-tetrahydropyridinoazole templates.
Medivir
5-Amino-oxazepine and 5-Amino-thiazepine Compounds as ß-Secretase Antagonists and Methods of Use: Patent Highlight.
TBA
BACE-Inhibitors: Potential Treatment of Alzheimer Disease, Dementia, and Related Neurodegenerative Diseases. C. Spiro-Heterocyclic Derivatives: Patent Highlight.
TBA
BACE Inhibitors: Potential Treatment of Alzheimer's Disease, Dementia, and Related Neurodegenerative Disorders (B): 3-Amino-4-fluoro-1H-isoindol Derivatives: Patent Highlight.
TBA
BACE Inhibitors: Potential Treatment of Alzheimer's Disease, Dementia, and Related Neurodegenerative Disorders (A): 5,6-Dihydroimidazo[1,2-a]pyrazin-8-yl-amine Derivatives: Patent Highlight.
TBA
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aß Reduction.
TBA
Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potentß-secretase inhibitors.
Purdue University
Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.
University Of South Florida
Novel BACE1 inhibitors possessing a 5-nitroisophthalic scaffold at the P2 position.
Kobe Gakuin 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
Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: design, synthesis and X-ray crystal structures of enzyme inhibitor complexes.
Link£Ping University
Discovery of cyclic sulfone hydroxyethylamines as potent and selectiveß-site APP-cleaving enzyme 1 (BACE1) inhibitors: structure-based design and in vivo reduction of amyloidß-peptides.
Novartis Pharma
BACE1 Inhibitor Peptides: Can an Infinitely Small k cat Value Turn the Substrate of an Enzyme into Its Inhibitor?
TBA
Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.
Envoy Therapeutics
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
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.
Merck Research Laboratories
Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.
Universitat De Barcelona
Fragment based drug discovery: practical implementation based on¹¿F NMR spectroscopy.
Amgen
Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.
Zhejiang University
Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.
Elan Pharmaceuticals
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.
Glaxosmithkline
Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening.
University Of Leeds
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.
University Of Florida
Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.
Elan Pharmaceuticals
BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens.
Gyeongsang National University School Of Medicine
Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.
Lg Life Sciences
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.
Schering-Plough Research Institute
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).
Glaxosmithkline
BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.
Kyoto Pharmaceutical University
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.
Wyeth Research
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.
Schering-Plough Research Institute
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
Discovery of a novel warhead against beta-secretase through fragment-based lead generation.
Astrazeneca R&D
Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity.
Johnson & Johnson Pharmaceutical Research And Development
Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method.
Johnson & Johnson Pharmaceutical Research And Development
Secretase targets for Alzheimer's disease: identification and therapeutic potential.
Harvard Medical School
The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not aß-secretase inhibitor.
Beijing Institute Of Pharmacology And Toxicology
Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design.
Kobe Gakuin University
Synthesis of monomeric derivatives to probe memoquin's bivalent interactions.
University Of Bologna
Structure-activity relationships for naturally occurring coumarins asß-secretase inhibitor.
Kinki University
A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.
Sissa-Isas
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.
Merck Research Laboratories
On a possible neutral charge state for the catalytic dyad inß-secretase when bound to hydroxyethylene transition state analogue inhibitors.
Universidad De Santiago De Compostela
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
Rational design and synthesis of aminopiperazinones asß-secretase (BACE) inhibitors.
Research Informatics & Integrative Genomics
Design, synthesis, and qualitative structure-activity evaluations of novelß-secretase inhibitors as potential Alzheimer's drug leads.
University Of Sharjah
Monosubstituted¿-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors ofß-secretase (BACE).
Bristol-Myers Squibb
Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.
Bristol-Myers Squibb Research And Development
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.
Pfizer
From fragment screening to in vivo efficacy: optimization of a series of 2-aminoquinolines as potent inhibitors of beta-site amyloid precursor protein cleaving enzyme 1 (BACE1).
Amgen
Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.
Kyoto Pharmaceutical University
Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.
Institut F£R Molekulare Physiologie
Triazole-linked reduced amide isosteres: an approach for the fragment-based drug discovery of anti-Alzheimer's BACE1 inhibitors.
Virginia Tech
Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay.
Singapore Polytechnic
Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on β-secretase (BACE-1).
Gyeongsang National University
Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.
Novartis Institutes For Biomedical Research
Synthesis and evaluation of arylquinones as BACE1 inhibitors,β-amyloid peptide aggregation inhibitors, and destabilizers of preformed β-amyloid fibrils.
Universidad Complutense
Investigation ofa-phenylnorstatine anda-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors.
Uppsala University
BACE1 inhibitory activities of enantiomerically pure, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulfonamides.
University Of Pisa
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.
Pfizer
Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors.
Singapore Polytechnic
Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.
Elan Pharmaceuticals
Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.
Elan Pharmaceuticals
Topsentinols, 24-isopropyl steroids from the marine sponge Topsentia sp.
University Of Hawaii At Manoa
Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.
University Of Bologna
Xestosaprols from the Indonesian marine sponge Xestospongia sp.
University Of Hawaii At Manoa
Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads.
Applied Science University
Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors.
Institute Of Science And Technology
Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity.
Pukyong National University
Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.
Johnson & Johnson Pharmaceutical Research & Development
Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.
Kyoto Pharmaceutical University
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.
Merck Research Laboratories
Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase.
Peking University
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth
SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.
Merck Research Laboratories
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.
Universit£
Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.
Link£Ping University
Biotransformation of isoimperatorin and imperatorin by Glomerella cingulata and beta-secretase inhibitory activity.
Kinki University
Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core.
Stockholm University
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.
Novartis Institutes For Biomedical Research
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.
Wyeth Research
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.
Merck Research Laboratories
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.
Wyeth Research
Application of fragment-based NMR screening, X-ray crystallography, structure-based design, and focused chemical library design to identify novel microM leads for the development of nM BACE-1 (beta-site APP cleaving enzyme 1) inhibitors.
Schering-Plough Research Institute
Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.
Schering-Plough Research Institute
P2'-truncated BACE-1 inhibitors with a novel hydroxethylene-like core.
Stockholm University
Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors.
University Of Sharjah
Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.
Uppsala University
Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1).
Technische Universit£T M£Nchen
Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.
Bristol-Myers Squibb Research And Development
Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.
Novartis Institutes For Biomedical Research
Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.
Merck Research Laboratories
Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold.
Kyoto Pharmaceutical University
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.
Purdue University
Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase.
Chinese Academy Of Sciences
Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.
University Of Illinois At Chicago
Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors.
Zhejiang University
Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.
LinköPing University
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.
Schering-Plough Research Institute
Tetramic and tetronic acids: an update on new derivatives and biological aspects.
University Of Bayreuth
Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.
Purdue University
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.
Glaxosmithkline
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.
Wyeth Research
Application of fragment-based lead generation to the discovery of novel, cyclic amidine beta-secretase inhibitors with nanomolar potency, cellular activity, and high ligand efficiency.
Astrazeneca Pharmaceuticals
Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.
TBA
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.
Merck Research Laboratories
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).
Technische UniversitäT MüNchen
beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.
Kyoto Pharmaceutical University
Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.
Kyoto Pharmaceutical University
BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline.
University Of The Mediterranean
Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations.
University Of ZüRich
Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.
Kyoto Pharmaceutical University
Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.
National Institute Of Health Sciences
Efficient evaluation of binding free energy using continuum electrostatics solvation.
University Of ZüRich
KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.
Kyoto Pharmaceutical University
Rational design and synthesis of selective BACE-1 inhibitors.
Merck Research Laboratories
KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.
Kyoto Pharmaceutical University
Green tea catechins as a BACE1 (beta-secretase) inhibitor.
Kyungpook National University
Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals
Bifunctional phenolic-choline conjugates as anti-oxidants and acetylcholinesterase inhibitors.
Instituto Superior Técnico
Synthesis and biological evaluation of polyhydroxy benzophenone as mushroom tyrosinase inhibitors.
Sun Yat-Sen University
Synthetic Triterpenoid Inhibition of Human Ghrelin O-Acyltransferase: The Involvement of a Functionally Required Cysteine Provides Mechanistic Insight into Ghrelin Acylation.
Syracuse University
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist.
Roche Bioscience
[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors.
Georgetown University
[35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents.
Institut De Recherches Servier
Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells.
Sanofi Recherche
Cholecystokinin receptors: biochemical demonstration and autoradiographical localization in rat brain and pancreas using [3H] cholecystokinin8 as radioligand.
F. Hoffmann-La Roche
Ligand binding to thromboxane receptors on human platelets: correlation with biological activity.
University Of Edinburgh
Characterization of 5-hydroxytryptamine1B receptors in rat spinal cord via [125I]iodocyanopindolol binding and inhibition of [3H]-5-hydroxytryptamine release.
University Of Texas
Neoglycopeptides as inhibitors of oligosaccharyl transferase: insight into negotiating product inhibition.
Massachusetts Institute Of Technology
Structure-based design and in-parallel synthesis of inhibitors of AmpC beta-lactamase.
Northwestern University
Energetic, structural, and antimicrobial analyses of beta-lactam side chain recognition by beta-lactamases.
Northwestern University
Identification of RIP1 kinase as a specific cellular target of necrostatins.
Tufts University
Preparation of (4,4-difluoro-1,2,3,4-tetrahydro-5H-1-benzazepin-5-ylidene)acetamide derivatives as novel arginine vasopressin V(2) receptor agonists.
Astellas Pharma
Structures of lung cancer-derived EGFR mutants and inhibitor complexes: mechanism of activation and insights into differential inhibitor sensitivity.
Harvard Medical School
Synthesis and biological evaluation of imidazo[1,2-a]pyridine derivatives as novel PI3 kinase p110alpha inhibitors.
Astellas Pharma
Synthesis and biological evaluation of sulfonylhydrazone-substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110alpha inhibitors.
Astellas Pharma
(3R,5S,E)-7-(4-(4-Fluorophenyl)-6-isopropyl-2-(methyl(1-methyl-1H-1,2,4-triazol-5-yl)amino)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoic Acid (BMS-644950): A Rationally Designed Orally Efficacious 3-Hydroxy-3-methylglutaryl Coenzyme-A Reductase Inhibitor with Reduced Myotoxicity Potential.
Bristol-Myers Squibb
A highly selective, non-hydantoin, non-carboxylic acid inhibitor of aldose reductase with potent oral activity in diabetic rat models: 6-(5-chloro-3-methylbenzofuran- 2-sulfonyl)-2-H-pyridazin-3-one.
Pfizer
Discovery of (1R,5S)-N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide (SCH 503034), a selective, potent, orally bioavailable hepatitis C virus NS3 protease inhibitor
Schering-Plough Research Institute
Discovery and preclinical profile of Saxagliptin (BMS-477118): a highly potent, long-acting, orally active dipeptidyl peptidase IV inhibitor for the treatment of type 2 diabetes.
Bristol-Myers Squibb Pharmaceutical Research Institute
1-imidazolyl(alkyl)-substituted di- and tetrahydroquinolines and analogues: syntheses and evaluation of dual inhibitors of thromboxane A(2) synthase and aromatase.
Universitat Des Saarlandes
Enantioselective nonsteroidal aromatase inhibitors identified through a multidisciplinary medicinal chemistry approach.
University Of Bologna
Cyclic sulfamide HIV-1 protease inhibitors, with sidechains spanning from P2/P2' to P1/P1'.
Uppsala University
Identification of tricyclic analogs related to ellagic acid as potent/selective tyrosine protein kinase inhibitors.
Pfizer
Novel azapeptide inhibitors of hepatitis C virus serine protease.
Boehringer Ingelheim (Canada)
Synthesis and anti-HIV-1 activity of a series of imidazo[1,5-b]pyridazines.
Glaxo Group Research