476 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
Recent advance on carbamate-based cholinesterase inhibitors as potential multifunctional agents against Alzheimer's disease.
Lanzhou University
beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.
Kyoto Pharmaceutical University
Cathepsin D inhibitors based on tasiamide B derivatives with cell membrane permeability.
Fudan University
Modulating physicochemical properties of tetrahydropyridine-2-amine BACE1 inhibitors with electron-withdrawing groups: A systematic study.
Janssen Research & Development
Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.
Kyoto Pharmaceutical University
Xanthenes in Medicinal Chemistry - Synthetic strategies and biological activities.
Ciimar
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
Advancements in the development of multi-target directed ligands for the treatment of Alzheimer's disease.
Central University Of Punjab
Resveratrol-based compounds and neurodegeneration: Recent insight in multitarget therapy.
"G. D'Annunzio" University Of Chieti-Pescara
Small molecules targeting ?-secretase and their potential biological applications.
Shenyang Pharmaceutical University
Therapeutic potential of quinazoline derivatives for Alzheimer's disease: A comprehensive review.
University Of Louisiana At Lafayette
Small molecule therapeutics for tauopathy in Alzheimer's disease: Walking on the path of most resistance.
Karolinska Institutet
Meroterpenoids produced by fungi: Occurrence, structural diversity, biological activities, and their molecular targets.
Guangzhou University Of Chinese Medicine
Sebetralstat (KVD900): A Potent and Selective Small Molecule Plasma Kallikrein Inhibitor Featuring a Novel P1 Group as a Potential Oral On-Demand Treatment for Hereditary Angioedema.
Kalvista Pharmaceuticals
Alzheimer's disease: Updated multi-targets therapeutics are in clinical and in progress.
Guizhou Medical University
A review on ferulic acid and analogs based scaffolds for the management of Alzheimer's disease.
Indian Institute Of Technology (Banaras Hindu University)
Glycogen Synthase Kinase 3?: A New Gold Rush in Anti-Alzheimer's Disease Multitarget Drug Discovery?
University Of Turin
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
Synthesis of the Potent, Selective, and Efficacious ?-Secretase (BACE1) Inhibitor NB-360.
TBA
Macrocyclic BACE1 inhibitors with hydrophobic cross-linked structures: Optimization of ring size and ring structure.
Kyoto Pharmaceutical University
Discovery of Umibecestat (CNP520): A Potent, Selective, and Efficacious ?-Secretase (BACE1) Inhibitor for the Prevention of Alzheimer's Disease.
Novartis Pharma
Efficient evaluation of binding free energy using continuum electrostatics solvation.
University Of ZüRich
A Brain-Penetrant and Bioavailable Pyrazolopiperazine BACE1 Inhibitor Elicits Sustained Reduction of Amyloid ? In Vivo.
Janssen Research & Development
Discovery and Early Clinical Development of LY3202626, a Low-Dose, CNS-Penetrant BACE Inhibitor.
Lilly Research Laboratories
Discovery of Extremely Selective Fused Pyridine-Derived ?-Site Amyloid Precursor Protein-Cleaving Enzyme (BACE1) Inhibitors with High In Vivo Efficacy through 10s Loop Interactions.
Shionogi Pharmaceutical Research Center
JNJ-67569762, A 2-Aminotetrahydropyridine-Based Selective BACE1 Inhibitor Targeting the S3 Pocket: From Discovery to Clinical Candidate.
Janssen Research & Development
From virtual screening hits targeting a cryptic pocket in BACE-1 to a nontoxic brain permeable multitarget anti-Alzheimer lead with disease-modifying and cognition-enhancing effects.
University Of Barcelona
Structure-activity relationship study of hydroxyethylamine isostere and P1' site structure of peptide mimetic BACE1 inhibitors.
Kyoto Pharmaceutical University
Inhibition of BACE1 and Amyloid-? Aggregation by Meroterpenoids from the Mushroom
Meiji Pharmaceutical University
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
Discovery of multifunctional anti-Alzheimer's agents with a unique mechanism of action including inhibition of the enzyme butyrylcholinesterase and ?-aminobutyric acid transporters.
Jagiellonian University Medical College
Structure-Based Approaches to Improving Selectivity through Utilizing Explicit Water Molecules: Discovery of Selective ?-Secretase (BACE1) Inhibitors over BACE2.
Shionogi Pharmaceutical Research Center
Green tea catechins as a BACE1 (beta-secretase) inhibitor.
Kyungpook National University
Balancing potency and basicity by incorporating fluoropyridine moieties: Discovery of a 1-amino-3,4-dihydro-2,6-naphthyridine BACE1 inhibitor that affords robust and sustained central A? reduction.
Shionogi Pharmaceutical Research Center
Synthesis and evaluation of multi-target-directed ligands with BACE-1 inhibitory and Nrf2 agonist activities as potential agents against Alzheimer's disease.
School Of Traditional Chinese Pharmacy
Discovery of Atabecestat (JNJ-54861911): A Thiazine-Based ?-Amyloid Precursor Protein Cleaving Enzyme 1 Inhibitor Advanced to the Phase 2b/3 EARLY Clinical Trial.
Janssen Research & Development
Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals
Centrally Active Multitarget Anti-Alzheimer Agents Derived from the Antioxidant Lead CR-6.
University Of Barcelona (Ub)
The development of a structurally distinct series of BACE1 inhibitors via the (Z)-fluoro-olefin amide bioisosteric replacement.
Amgen
Sulfoximines as Rising Stars in Modern Drug Discovery? Current Status and Perspective on an Emerging Functional Group in Medicinal Chemistry.
Endotherm
Design, synthesis, and multitargeted profiling of N-benzylpyrrolidine derivatives for the treatment of Alzheimer's disease.
Indian Institute Of Technology (Banaras Hindu University)
Design and development of molecular hybrids of 2-pyridylpiperazine and 5-phenyl-1,3,4-oxadiazoles as potential multifunctional agents to treat Alzheimer's disease.
Indian Institute Of Technology (Banaras Hindu University)
Discovery of Orally Active Hydroxyethylamine Based SPPL2a Inhibitors.
Novartis Institutes For Biomedical Research
3,3-Difluoro-3,4,5,6-tetrahydropyridin-2-amines: Potent and permeable BACE-1 inhibitors.
Janssen Research & Development
Synthesis of morpholine derivatives using the Castagnoli-Cushman reaction as BACE1 inhibitors: Unexpected binding activity of cyclic thioamides.
University Of Florence
The Medicinal Chemistry in the Era of Machines and Automation: Recent Advances in Continuous Flow Technology.
University Of Perugia
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints.
Eli Lilly
Design and development of multitarget-directed N-Benzylpiperidine analogs as potential candidates for the treatment of Alzheimer's disease.
Indian Institute Of Technology (Banaras Hindu University)
Discovery of S3-Truncated, C-6 Heteroaryl Substituted Aminothiazine ?-Site APP Cleaving Enzyme-1 (BACE1) Inhibitors.
Bristol-Myers Squibb
4-Aryl Pyrrolidines as a Novel Class of Orally Efficacious Antimalarial Agents. Part 1: Evaluation of 4-Aryl- N-benzylpyrrolidine-3-carboxamides.
Saint Louis University
Advancement of multi-target drug discoveries and promising applications in the field of Alzheimer's disease.
Jining Medical University
Tricyclic Inhibitors of ?-Secretase and Their Methods of Use for the Treatment of Alzheimer's Disease.
Temple University School Of Pharmacy
1-Benzylpyrrolidine-3-amine-based BuChE inhibitors with anti-aggregating, antioxidant and metal-chelating properties as multifunctional agents against Alzheimer's disease.
Jagiellonian University Medical College
Triazole derivatives as inhibitors of Alzheimer's disease: Current developments and structure-activity relationships.
Wuhan Institute Of Technology
Design, synthesis and evaluation of 2-amino-imidazol-4-one derivatives as potent ?-site amyloid precursor protein cleaving enzyme 1 (BACE-1) inhibitors.
Nanjing University Of Chinese Medicine
Cinnamamide: An insight into the pharmacological advances and structure-activity relationships.
National Institute Of Pharmaceutical Education And Research (Niper)
Multi-target design strategies for the improved treatment of Alzheimer's disease.
China Pharmaceutical University
Discovery of AM-6494: A Potent and Orally Efficacious ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor with in Vivo Selectivity over BACE2.
TBA
Anti-cholinesterase hybrids as multi-target-directed ligands against Alzheimer's disease (1998-2018).
Csir-Central Drug Research Institute
New evolutions in the BACE1 inhibitor field from 2014 to 2018.
Janssen Research & Development
Design, synthesis, and biological evaluation of novel 4-oxobenzo[d]1,2,3-triazin-benzylpyridinum derivatives as potent anti-Alzheimer agents.
University Of Zanjan
Synthesis and evaluation of tetrahydroisoquinoline-benzimidazole hybrids as multifunctional agents for the treatment of Alzheimer's disease.
Sun Yat-Sen University
Meroterpenoids with BACE1 Inhibitory Activity from the Fruiting Body of
Meiji Pharmaceutical University
Multi-target-directed-ligands acting as enzyme inhibitors and receptor ligands.
Julius Maximilian University Of W£Rzburg
Discovery of an Extremely Potent Thiazine-Based ?-Secretase Inhibitor with Reduced Cardiovascular and Liver Toxicity at a Low Projected Human Dose.
TBA
Bioactivity-guided identification of flavonoids with cholinesterase and ?-amyloid peptide aggregation inhibitory effects from the seeds of Millettia pachycarpa.
Sichuan University
Evaluation of a Series of ?-Secretase 1 Inhibitors Containing Novel Heteroaryl-Fused-Piperazine Amidine Warheads.
Janssen Research & Development
Synthesis and evaluation of curcumin derivatives toward an inhibitor of beta-site amyloid precursor protein cleaving enzyme 1.
Yamagata University
Structure-activity relationship study of BACE1 inhibitors possessing a chelidonic or 2,6-pyridinedicarboxylic scaffold at the P(2) position.
Kobe Gakuin University
Design and synthesis of novel 3,5-bis-N-(aryl/heteroaryl) carbamoyl-4-aryl-1,4-dihydropyridines as small molecule BACE-1 inhibitors.
Shiraz University Of Medical Sciences
Conformational restriction approach to ?-secretase (BACE1) inhibitors III: effective investigation of the binding mode by combinational use of X-ray analysis, isothermal titration calorimetry and theoretical calculations.
Hokkaido University
Structure-based design of ?-site APP cleaving enzyme 1 (BACE1) inhibitors for the treatment of Alzheimer's disease.
Vitae Pharmaceuticals
Conformational restriction approach to BACE1 inhibitors II: SAR study of the isocytosine derivatives fixed with a cis-cyclopropane ring.
Shionogi
Core refinement toward permeable ?-secretase (BACE-1) inhibitors with low hERG activity.
Astrazeneca
Structure-Based Design of Selective ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitors: Targeting the Flap to Gain Selectivity over BACE2.
TBA
Overcoming Time-Dependent Inhibition (TDI) of Cytochrome P450 3A4 (CYP3A4) Resulting from Bioactivation of a Fluoropyrimidine Moiety.
TBA
Multi-target-directed ligands for Alzheimer's disease: Discovery of chromone-based monoamine oxidase/cholinesterase inhibitors.
University Of Porto
Donepezil-based multi-functional cholinesterase inhibitors for treatment of Alzheimer's disease.
China Pharmaceutical University
A phenotypic approach to the discovery of compounds that promote non-amyloidogenic processing of the amyloid precursor protein: Toward a new profile of indirect ?-secretase inhibitors.
Universit£
Design, synthesis, X-ray studies, and biological evaluation of novel BACE1 inhibitors with bicyclic isoxazoline carboxamides as the P3 ligand.
Purdue University
Discovery of Potent and Centrally Active 6-Substituted 5-Fluoro-1,3-dihydro-oxazine ?-Secretase (BACE1) Inhibitors via Active Conformation Stabilization.
TBA
BACE1 Inhibitory Meroterpenoids from Aspergillus terreus.
Huazhong University Of Science And Technology
Rational Design of Novel 1,3-Oxazine Based ?-Secretase (BACE1) Inhibitors: Incorporation of a Double Bond To Reduce P-gp Efflux Leading to Robust A? Reduction in the Brain.
TBA
Mapping the Efficiency and Physicochemical Trajectories of Successful Optimizations.
Glaxosmithkline
Multipotent AChE and BACE-1 inhibitors for the treatment of Alzheimer's disease: Design, synthesis and bio-analysis of 7-amino-1,4-dihydro-2H-isoquilin-3-one derivates.
Central South University
Discovery of imidazopyridines containing isoindoline-1,3-dione framework as a new class of BACE1 inhibitors: Design, synthesis and SAR analysis.
University Of Tehran
Diastereoselective synthesis of fused cyclopropyl-3-amino-2,4-oxazine ?-amyloid cleaving enzyme (BACE) inhibitors and their biological evaluation.
Amgen
Design and Synthesis of Clinical Candidate PF-06751979: A Potent, Brain Penetrant, ?-Site Amyloid Precursor Protein Cleaving Enzyme 1 (BACE1) Inhibitor Lacking Hypopigmentation.
Pfizer
Novel multi-target compounds in the quest for new chemotherapies against Alzheimer's disease: An experimental and theoretical study.
The City University Of New York (Cuny)
Novel tetrahydrocarbazole benzyl pyridine hybrids as potent and selective butryl cholinesterase inhibitors with neuroprotective and ?-secretase inhibition activities.
Tehran University Of Medical Sciences
Isolation, Synthesis, and Antisepsis Effects of a C-Methylcoumarinochromone Isolated from Abronia nana Cell Culture.
Kyungpook National University
Optimization of 1,4-Oxazine ?-Secretase 1 (BACE1) Inhibitors Toward a Clinical Candidate.
Janssen Pharmaceutica
Multifunctional iminochromene-2H-carboxamide derivatives containing different aminomethylene triazole with BACE1 inhibitory, neuroprotective and metal chelating properties targeting Alzheimer's disease.
Shiraz University Of Medical Sciences
Discovery of amino-1,4-oxazines as potent BACE-1 inhibitors.
Novartis Institutes For Biomedical Research
2-Substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamides as BACE1 inhibitors: Synthesis, biological evaluation and docking studies.
Peking University Health Science Center
Synthesis, docking study and neuroprotective effects of some novel pyrano[3,2-c]chromene derivatives bearing morpholine/phenylpiperazine moiety.
Tehran University Of Medical Sciences
BACE1 inhibitory activity and molecular docking analysis of meroterpenoids from Sargassum serratifolium.
Pukyong National University
Design and synthesis of bicyclic acetals as Beta Secretase (BACE1) inhibitors.
University Of Florence
Aminomethyl-Derived Beta Secretase (BACE1) Inhibitors: Engaging Gly230 without an Anilide Functionality.
The Scripps Research Institute
Design, synthesis and SAR analysis of potent BACE1 inhibitors: Possible lead drug candidates for Alzheimer's disease.
University Of Sharjah
Optimization of Hydroxyethylamine Transition State Isosteres as Aspartic Protease Inhibitors by Exploiting Conformational Preferences.
Eli Lilly
BACE-1 Inhibitors: From Recent Single-Target Molecules to Multitarget Compounds for Alzheimer's Disease.
University Of Dundee
Lodopyridones B and C from a marine sediment-derived bacterium Saccharomonospora sp.
Ewha Womans University
Chromone as a Privileged Scaffold in Drug Discovery: Recent Advances.
University Of Porto
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands.
Purdue University
Design, synthesis and SAR study of hydroxychalcone inhibitors of human ß-secretase (BACE1).
Shanghai Institute Of Material Medica, Chinese Academy Of Sciences
Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.
Tehran University Of Medical Sciences
Synthesis of tetramic and tetronic acids as beta-secretase inhibitors.
Darmstadt Technical University
Synthesis, in vitro Biological Evaluation and Molecular Docking Studies of Benzimidamides as Potential BACE1 Inhibitors.
Peking University Health Science Center
The discovery of novel β-secretase inhibitors: pharmacophore modeling, virtual screening, and docking studies.
Peking University Health Science Center
Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.
Gsk
Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.
Gsk
Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.
Gsk
BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.
Gsk
Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.
Gsk
Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.
Merck Research Laboratories
Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.
Merck Research Laboratories
2-Amino-3,4-dihydroquinazolines as Inhibitors of BACE-1 (beta-Site APP Cleaving Enzyme): Use of Structure Based Design to Convert a Micromolar Hit into a Nanomolar Lead.
Johnson & Johnson Pharmaceutical
Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).
University Of Illinois At Chicago
Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals
Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays.
Universite De La Mediterranee
Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.
Merck Research Laboratories
Evaluating scoring functions for docking and designing beta-secretase inhibitors.
Merck Research Laboratories
Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.
Merck Research Laboratories
BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.
Merck Research Laboratories
Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.
Merck Research Laboratories
Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).
Merck Research Laboratories
Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).
University Of Illinois At Chicago
Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.
Purdue University
Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.
Purdue University
Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.
Merck Research Laboratories
Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).
Merck Research Laboratories
Conformationally biased P3 amide replacements of beta-secretase inhibitors.
Merck Research Laboratories
Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex.
Eli Lilly
Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.
Elan Pharmaceuticals