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327 articles for thisTarget


The following articles (labelled with PubMed ID or TBD) are for your review
PMIDDataArticle TitleOrganization
27721153 18 Design, synthesis and biological evaluation of new phthalimide and saccharin derivatives with alicyclic amines targeting cholinesterases, beta-secretase and amyloid beta aggregation.EBI Jagiellonian University Medical College
28043778 3 Neuritogenic activity of bi-functional bis-tryptoline triazole.EBI Chiang Mai University
27816517 14 Discovery of furo[2,3-d][1,3]thiazinamines as beta amyloid cleaving enzyme-1 (BACE1) inhibitors.EBI Bristol-Myers Squibb
27104967 1 Pregnane-10,2-carbolactones from a Hawaiian Marine Sponge in the Genus Myrmekioderma.EBI University of Hawaii at Manoa
27046190 10 Impact of Binding Site Comparisons on Medicinal Chemistry and Rational Molecular Design.EBI TU Dortmund University
27211244 9 Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium.EBI University of Florida
26978477 25 Fragment-Linking Approach Using (19)F NMR Spectroscopy To Obtain Highly Potent and Selective Inhibitors of▀-Secretase.EBI Amgen, Inc.
26985314 23 Targeting the BACE1 Active Site Flap Leads to a Potent Inhibitor That Elicits Robust Brain A▀ Reduction in Rodents.EBI Bristol-Myers Squibb Company
26937601 55 Structure-Based Design of an Iminoheterocyclic▀-Site Amyloid Precursor Protein Cleaving Enzyme (BACE) Inhibitor that Lowers Central A▀ in Nonhuman Primates.EBI Merck Research Laboratories
27102162 1 Design, synthesis and in vitro evaluation studies of sulfonyl-amino-acetamides as small molecule BACE-1 inhibitors.EBI Birla Institute of Technology and Science Pilani
26696252 32 Versatility of the Curcumin Scaffold: Discovery of Potent and Balanced Dual BACE-1 and GSK-3▀ Inhibitors.EBI Alma Mater Studiorum - University of Bologna
26632651 70 Novel Tacrine-Benzofuran Hybrids as Potent Multitarget-Directed Ligands for the Treatment of Alzheimer's Disease: Design, Synthesis, Biological Evaluation, and X-ray Crystallography.EBI China Pharmaceutical University
26608551 35 Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities.EBI Korea University of Science and Technology
26614409 1 Rational design, synthesis and in vitro evaluation of allylidene hydrazinecarboximidamide derivatives as BACE-1 inhibitors.EBI Birla Institute of Technology and Science Pilani
26378740 37 1,4-Oxazine▀-Secretase 1 (BACE1) Inhibitors: From Hit Generation to Orally Bioavailable Brain Penetrant Leads.EBI Janssen Pharmaceutica NV
26497283 68 Macrocyclic prolinyl acyl guanidines as inhibitors of▀-secretase (BACE).EBI Bristol-Myers Squibb Company
26264846 15 Evaluation of transition-state mimics in a superior BACE1 cleavage sequence as peptide-mimetic BACE1 inhibitors.EBI Kyoto Pharmaceutical University
26003339 12 From AChE to BACE1 inhibitors: The role of the amine on the indanone scaffold.EBI University of Bologna
25167370 75 Transition state mimetics of the Plasmodium export element are potent inhibitors of Plasmepsin V from P. falciparum and P. vivax.EBI The Walter and Eliza Hall Institute of Medical Research
26061085 13 Peptidomimetic▀-Secretase Inhibitors Comprising a Sequence of Amyloid-▀ Peptide for Alzheimer's Disease.EBI Instituto de Biologia Experimental e Tecnol£gica
26003344 48 Isolation of cholinesterase and▀-secretase 1 inhibiting compounds from Lycopodiella cernua.EBI Catholic University of Daegu
26001341 19 Preparation and biological evaluation of conformationally constrained BACE1 inhibitors.EBI Lilly Research Laboratories
25941546 9 4,6-Diarylaminothiazines as BACE1 Inhibitors and Their Use for the Reduction of Beta-Amyloid Production.EBI Temple University School of Pharmacy
25781223 96 Utilizing structures of CYP2D6 and BACE1 complexes to reduce risk of drug-drug interactions with a novel series of centrally efficacious BACE1 inhibitors.EBI The Scripps Research Institute
25695670 35 Discovery of a series of efficient, centrally efficacious BACE1 inhibitors through structure-based drug design.EBI Eurofarma Laboratorios S.A.
25842365 21 Design, synthesis and biological evaluation of tasiamide B derivatives as BACE1 inhibitors.EBI Fudan University
25782742 76 trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker.EBI Novartis Pharma AG
25754490 44 trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker.EBI Novartis Pharma AG
25728416 25 Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors.EBI Merck Research Laboratories
25736996 1 Novel▀-amyloid aggregation inhibitors possessing a turn mimic.EBI Kobe Pharmaceutical University
25699151 57 An Orally Available BACE1 Inhibitor That Affords Robust CNS A▀ Reduction without Cardiovascular Liabilities.EBI Amgen Inc.
25613679 79 Development of 2-aminooxazoline 3-azaxanthenes as orally efficacious▀-secretase inhibitors for the potential treatment of Alzheimer's disease.EBI Amgen Inc.
25088549 47 Syntheses of coumarin-tacrine hybrids as dual-site acetylcholinesterase inhibitors and their activity against butylcholinesterase, A▀ aggregation, and▀-secretase.EBI Central China Normal University
25050166 58 Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors.EBI Novartis Institutes for BioMedical Research
25537272 17 Structure-based design, synthesis and biological evaluation of novel▀-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand.EBI Purdue University
25455483 61 Discovery of potent iminoheterocycle BACE1 inhibitors.EBI Merck Research Laboratories
25411915 54 8-Tetrahydropyran-2-yl chromans: highly selective beta-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors.EBI Array BioPharma
25389560 96 Lead optimization and modulation of hERG activity in a series of aminooxazoline xanthene▀-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.EBI Amgen Inc.
25363711 62 Inhibitors of▀-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).EBI Amgen, Inc.
24921156 6 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.EBI University of Coimbra
24835197 13 ▀-Secretase (BACE1)-inhibiting C-methylrotenoids from Abronia nana suspension cultures.EBI Kyungpook National University
24780121 19 Synthesis, characterization, and PK/PD studies of a series of spirocyclic pyranochromene BACE1 inhibitors.EBI Genentech Inc.
24704031 69 The evolution of amidine-based brain penetrant BACE1 inhibitors.EBI Janssen Research and Development
24568372 40 Synthesis and multitarget biological profiling of a novel family of rhein derivatives as disease-modifying anti-Alzheimer agents.EBI Universitat de Barcelona
24763262 8 4-Oxo-1,4-dihydro-quinoline-3-carboxamides as BACE-1 inhibitors: synthesis, biological evaluation and docking studies.EBI Peking University Health Science Center
23590342 105 ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease.EBI F. Hoffmann-La Roche Ltd
23537249 165 Spirocyclicß-site amyloid precursor protein cleaving enzyme 1 (BACE1) inhibitors: from hit to lowering of cerebrospinal fluid (CSF) amyloidß in a higher species.EBI Array BioPharma
23480856 22 Phenylimino-2H-chromen-3-carboxamide derivatives as novel small molecule inhibitors ofß-secretase (BACE1).EBI Tehran University of Medical Sciences
23465612 17 Structure-based design of novel dihydroisoquinoline BACE-1 inhibitors that do not engage the catalytic aspartates.EBI Elan Pharmaceuticals
23425156 24 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.EBI Novartis Pharma AG
23374014 24 Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design.EBI University of Leeds
23360239 19 A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore.EBI Novartis Pharma AG
23219701 1 Discovery of alkenylboronic acids as neuroprotective agents affecting multiple biological targets involved in Alzheimer's disease.EBI Universidad Complutense
23218605 17 Novel peptidomimetics as BACE-1 inhibitors: synthesis, molecular modeling, and biological studies.EBI Universit£ degli Studi di Siena
22325942 31 Aminoimidazoles as BACE-1 inhibitors: the challenge to achieve in vivo brain efficacy.EBI AstraZeneca
21093114 61 Self-organizing molecular field analysis on humanß-secretase nonpeptide inhibitors: 5, 5-disubstituted aminohydantoins.EBI Sichuan University
21381769 56 Macrocycles are great cycles: applications, opportunities, and challenges of synthetic macrocycles in drug discovery.EBI Universite£ de Sherbrooke
23181502 57 Cyanobacterial peptides as a prototype for the design of potentß-secretase inhibitors and the development of selective chemical probes for other aspartic proteases.EBI University of Florida
23030502 86 Acyl guanidine inhibitors ofß-secretase (BACE-1): optimization of a micromolar hit to a nanomolar lead via iterative solid- and solution-phase library synthesis.EBI Bristol-Myers Squibb Research
23017051 69 New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain.EBI AstraZeneca
22989333 43 Design and validation of bicyclic iminopyrimidinones as beta amyloid cleaving enzyme-1 (BACE1) inhibitors: conformational constraint to favor a bioactive conformation.EBI Merck Research Laboratories
22984865 43 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.EBI Pfizer Inc.
22954357 29 Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure.EBI Purdue University
22928914 104 Structure- and property-based design of aminooxazoline xanthenes as selective, orally efficacious, and CNS penetrable BACE inhibitors for the treatment of Alzheimer's disease.EBI Amgen Inc.
22924815 97 Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides.EBI AstraZeneca
22468999 20 Discovery and optimization of a novel spiropyrrolidine inhibitor ofß-secretase (BACE1) through fragment-based drug design.EBI Pfizer Inc.
22468684 76 Design and synthesis of potent, orally efficacious hydroxyethylamine derivedß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors.EBI Amgen Inc.
22468639 26 Design and preparation of a potent series of hydroxyethylamine containingß-secretase inhibitors that demonstrate robust reduction of centralß-amyloid.EBI Amgen Inc.
22998419 47 Conformational restriction approach toß-secretase (BACE1) inhibitors: effect of a cyclopropane ring to induce an alternative binding mode.EBI Shionogi& Co., Ltd.
22506484 6 Structural modifications that alter the P-glycoprotein efflux properties of compounds.EBI Envoy Therapeutics
23041347 33 Design, synthesis, and bioevaluation of benzamides: novel acetylcholinesterase inhibitors with multi-functions on butylcholinesterase, Aß aggregation, andß-secretase.EBI Central China Normal University
23010268 32 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.EBI Medivir AB
22863204 17 Structure-based design, synthesis, and biological evaluation of dihydroquinazoline-derived potentß-secretase inhibitors.EBI Purdue University
22727644 43 Synthesis and structure-activity relationship studies of 1,3-disubstituted 2-propanols as BACE-1 inhibitors.EBI University of South Florida
22409666 4 Modern phenotypic drug discovery is a viable, neoclassic pharma strategy.EBI Lilly Research Laboratories
22726930 7 Novel BACE1 inhibitors possessing a 5-nitroisophthalic scaffold at the P2 position.EBI Kobe Gakuin University
22704921 34 Development and evaluation of multifunctional agents for potential treatment of Alzheimer's disease: application to a pyrimidine-2,4-diamine template.EBI University of Waterloo
22698785 28 Highly potent macrocyclic BACE-1 inhibitors incorporating a hydroxyethylamine core: design, synthesis and X-ray crystal structures of enzyme inhibitor complexes.EBI Link£ping University
22380629 174 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.EBI Novartis Pharma AG
22572583 49 Structure guided P1' modifications of HEA derivedß-secretase inhibitors for the treatment of Alzheimer's disease.EBI Envoy Therapeutics
22243648 112 New tacrine-4-oxo-4H-chromene hybrids as multifunctional agents for the treatment of Alzheimer's disease, with cholinergic, antioxidant, andß-amyloid-reducing properties.EBI Instituto de Qu£mica M£dica
22390835 80 Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor.EBI Merck Research Laboratories
22185619 50 Huprine-tacrine heterodimers as anti-amyloidogenic compounds of potential interest against Alzheimer's and prion diseases.EBI Universitat de Barcelona
22165820 22 Fragment based drug discovery: practical implementation based on¹¿F NMR spectroscopy.EBI Amgen, Inc.
20620068 8 Dual-target-directed 1,3-diphenylurea derivatives: BACE 1 inhibitor and metal chelator against Alzheimer's disease.EBI Zhejiang University
20634069 42 Improving the permeability of the hydroxyethylamine BACE-1 inhibitors: structure-activity relationship of P2' substituents.EBI Elan Pharmaceuticals
20598535 21 beta-Secretase (BACE-1) inhibitory effect of biflavonoids.EBI Shujitsu University
20579874 150 BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296.EBI GlaxoSmithKline R&D
19854048 3 Discovery of novel non-peptide inhibitors of BACE-1 using virtual high-throughput screening.EBI University of Leeds
20045648 39 Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors.EBI Wyeth Research
19715320 87 Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation.EBI University of Florida
19811916 83 Design and synthesis of cell potent BACE-1 inhibitors: structure-activity relationship of P1' substituents.EBI Elan Pharmaceuticals
18565755 8 BACE1 inhibitory effects of lavandulyl flavanones from Sophora flavescens.EBI Gyeongsang National University School of Medicine
18434152 64 Synthesis, SAR, and X-ray structure of human BACE-1 inhibitors with cyclic urea derivatives.EBI LG Life Sciences
17980584 72 Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor.EBI Schering-Plough Research Institute
18171614 63 BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs).EBI GlaxoSmithKline R&D
18226904 8 Tyramine fragment binding to BACE-1.EBI F. Hoffmann-La Roche
18249539 6 BACE1 inhibitors: optimization by replacing the P1' residue with non-acidic moiety.EBI Kyoto Pharmaceutical University
18068983 51 Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1' substrate binding pocket.EBI Wyeth Research
18023580 50 Potent pyrrolidine- and piperidine-based BACE-1 inhibitors.EBI Schering-Plough Research Institute
17998161 19 Multi-target-directed coumarin derivatives: hAChE and BACE1 inhibitors as potential anti-Alzheimer compounds.EBI University of Bologna
18181565 71 Multi-target-directed ligands to combat neurodegenerative diseases.EBI University of Bologna
17985861 5 Discovery of a novel warhead against beta-secretase through fragment-based lead generation.EBI AstraZeneca R&D
15341936 17 Modeling the binding affinities of beta-secretase inhibitors: application to subsite specificity.EBI Johnson& Johnson Pharmaceutical Research and Development
12747779 13 Calculation of the binding affinity of beta-secretase inhibitors using the linear interaction energy method.EBI Johnson& Johnson Pharmaceutical Research and Development
11784130 42 Design of substrate-based inhibitors of human beta-secretase.EBI TBA
11405641 8 Secretase targets for Alzheimer's disease: identification and therapeutic potential.EBI Harvard Medical School
14684336 20 P3 cap modified Phe*-Ala series BACE inhibitors.EBI Lilly Research Laboratories
14684335 21 Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR.EBI Lilly Research Laboratories
14643321 31 Design and synthesis of statine-containing BACE inhibitors.EBI Eli Lilly and Company
22225636 11 The green tea polyphenol (2)-epigallocatechin-3-gallate (EGCG) is not aß-secretase inhibitor.EBI Beijing Institute of Pharmacology and Toxicology
22178553 10 Tripeptidic BACE1 inhibitors devised by in-silico conformational structure-based design.EBI Kobe Gakuin University
22054058 22 Synthesis of monomeric derivatives to probe memoquin's bivalent interactions.EBI University of Bologna
22222157 55 Structure-activity relationships for naturally occurring coumarins asß-secretase inhibitor.EBI Kinki University
22209418 5 A small chemical library of 2-aminoimidazole derivatives as BACE-1 inhibitors: Structure-based design, synthesis, and biological evaluation.EBI Statistical and Biological Physics Sector, SISSA-ISAS, Via Bonomea 265, 34136 Trieste, Italy.
22130130 19 Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency.EBI Merck Research Laboratories
21452857 6 On a possible neutral charge state for the catalytic dyad inß-secretase when bound to hydroxyethylene transition state analogue inhibitors.EBI Universidad de Santiago de Compostela
22019465 28 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.EBI Zhejiang University
22071305 24 Rational design and synthesis of aminopiperazinones asß-secretase (BACE) inhibitors.EBI Research Informatics& Integrative Genomics
22044119 84 Design, synthesis, and qualitative structure-activity evaluations of novelß-secretase inhibitors as potential Alzheimer's drug leads.EBI University of Sharjah
21992804 1 Daedalols A-C, fungal-derived BACE1 inhibitors.EBI University of Hawai'i at Manoa
21782431 95 Monosubstituted¿-lactam and conformationally constrained 1,3-diaminopropan-2-ol transition-state isostere inhibitors ofß-secretase (BACE).EBI Bristol-Myers Squibb
21974952 31 Synthesis and in vivo evaluation of cyclic diaminopropane BACE-1 inhibitors.EBI Bristol-Myers Squibb Research and Development
21986588 19 Carbazole-containing arylcarboxamides as BACE1 inhibitors.EBI Universit£ di Pisa
21835615 165 New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region.EBI Pfizer Inc.
21707077 54 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).EBI Amgen Inc.
21803585 12 Structure-guided design and synthesis of P1' position 1-phenylcycloalkylamine-derived pentapeptidic BACE1 inhibitors.EBI Kyoto Pharmaceutical University
21798635 32 Multi-target strategy to address Alzheimer's disease: design, synthesis and biological evaluation of new tacrine-based dimers.EBI Institut f£r Molekulare Physiologie
21621412 6 Triazole-linked reduced amide isosteres: an approach for the fragment-based drug discovery of anti-Alzheimer's BACE1 inhibitors.EBI Virginia Tech
19447035 16 Novel non-peptide beta-secretase inhibitors derived from structure-based virtual screening and bioassay.EBI Singapore Polytechnic
21511472 13 Inhibition and structural reliability of prenylated flavones from the stem bark of Morus lhou on β-secretase (BACE-1).EBI Gyeongsang National University
21388807 45 Structure based design, synthesis and SAR of cyclic hydroxyethylamine (HEA) BACE-1 inhibitors.EBI Novartis Institutes for BioMedical Research
21441028 18 Synthesis and evaluation of arylquinones as BACE1 inhibitors,β-amyloid peptide aggregation inhibitors, and destabilizers of preformed β-amyloid fibrils.EBI Universidad Complutense
21112780 30 Design and synthesis of potent macrocyclic renin inhibitors.EBI Medivir AB
21183353 27 Investigation ofa-phenylnorstatine anda-benzylnorstatine as transition state isostere motifs in the search for new BACE-1 inhibitors.EBI Uppsala University
20934348 8 BACE1 inhibitory activities of enantiomerically pure, variously substituted N-(3-(4-benzhydrylpiperazin-1-yl)-2-hydroxypropyl) arylsulfonamides.EBI University of Pisa
20943389 2 Triazolyl tryptoline derivatives asß-secretase inhibitors.EBI Mahidol University
20880704 200 Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability.EBI Pfizer Inc.
20850315 17 Molecular docking and structure-activity relationship studies on benzothiazole based non-peptidic BACE-1 inhibitors.EBI Singapore Polytechnic
20833041 40 Design of an orally efficacious hydroxyethylamine (HEA) BACE-1 inhibitor in a preclinical animal model.EBI Elan Pharmaceuticals
20822903 87 Design and synthesis of hydroxyethylamine (HEA) BACE-1 inhibitors: structure-activity relationship of the aryl region.EBI Elan Pharmaceuticals
20806907 1 Topsentinols, 24-isopropyl steroids from the marine sponge Topsentia sp.EBI University of Hawaii at Manoa
20656487 45 Fragment-based discovery and optimization of BACE1 inhibitors.EBI Evotec UK Ltd
20420456 6 Polyamines in drug discovery: from the universal template approach to the multitarget-directed ligand design strategy.EBI University of Bologna
20503979 9 Xestosaprols from the Indonesian marine sponge Xestospongia sp.EBI University of Hawaii at Manoa
20378363 135 Elaborate ligand-based pharmacophore exploration and QSAR analysis guide the synthesis of novel pyridinium-based potent beta-secretase inhibitory leads.EBI Applied Science University
20303626 33 Design and synthesis of 1,4-dihydropyridine derivatives as BACE-1 inhibitors.EBI Institute of Science and Technology
20462757 15 Molecular docking studies of phlorotannins from Eisenia bicyclis with BACE1 inhibitory activity.EBI Pukyong National University
20399652 22 Macrocyclic BACE inhibitors: Optimization of a micromolar hit to nanomolar leads.EBI Johnson& Johnson Pharmaceutical Research& Development
20381362 8 Design of pentapeptidic BACE1 inhibitors with carboxylic acid bioisosteres at P1' and P4 positions.EBI Kyoto Pharmaceutical University
20347593 76 Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization.EBI Merck Research Laboratories
20153560 10 Synthesis and preliminary evaluation of peptidomimetic inhibitors of human beta-secretase.EBI Peking University
20223661 48 Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors.EBI Princ
20202842 47 Pyridinyl aminohydantoins as small molecule BACE1 inhibitors.EBI Wyeth Research
20176482 42 SAR of tertiary carbinamine derived BACE1 inhibitors: role of aspartate ligand amine pKa in enzyme inhibition.EBI Merck Research Laboratories
20172717 35 Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors.EBI Universit£ de Montr£al
20036448 20 Synthesis of potent BACE-1 inhibitors incorporating a hydroxyethylene isostere as central core.EBI Link£ping University
19939683 7 Biotransformation of isoimperatorin and imperatorin by Glomerella cingulata and beta-secretase inhibitory activity.EBI Kinki University
20128595 24 Design and synthesis of potent and selective BACE-1 inhibitors.EBI Stockholm University
20122837 21 Discovery of potent BACE-1 inhibitors containing a new hydroxyethylene (HE) scaffold: exploration of P1' alkoxy residues and an aminoethylene (AE) central core.EBI Stockholm University
19963375 30 Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application.EBI Novartis Institutes for BioMedicalResearch
19959359 46 Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors.EBI Wyeth Research
19968289 201 Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors.EBI Wyeth Research
19640712 5 A conformational constraint improves a beta-secretase inhibitor but for an unexpected reason.EBI Merck Research Laboratories
19757823 98 Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors.EBI Wyeth Research
20043700 5 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.EBI Schering-Plough Research Institute
20043696 17 Discovery of cyclic acylguanidines as highly potent and selective beta-site amyloid cleaving enzyme (BACE) inhibitors: Part I--inhibitor design and validation.EBI Schering-Plough Research Institute
19995674 17 P2'-truncated BACE-1 inhibitors with a novel hydroxethylene-like core.EBI Stockholm University
19788239 8 Rational design and synthesis of potent dibenzazepine motifs as beta-secretase inhibitors.EBI University of Sharjah
19576765 15 Design and synthesis of BACE-1 inhibitors utilizing a tertiary hydroxyl motif as the transition state mimic.EBI Uppsala University
19523824 3 Prolonged stability by cyclization: Macrocyclic phosphino dipeptide isostere inhibitors of beta-secretase (BACE1).EBI Technische Universit£t M£nchen
19375914 116 Synthesis and SAR of hydroxyethylamine based phenylcarboxyamides as inhibitors of BACE.EBI Bristol-Myers Squibb Research and Development
19195887 18 Macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors with activity in vivo.EBI Novartis Institutes for BioMedical Research
19409780 11 Discovery of aminoheterocycles as a novel beta-secretase inhibitor class: pH dependence on binding activity part 1.EBI Merck Research Laboratories
19345096 10 Significance of interactions of BACE1-Arg235 with its ligands and design of BACE1 inhibitors with P2 pyridine scaffold.EBI Kyoto Pharmaceutical University
19323561 11 Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease.EBI Purdue University
19162488 57 Design, synthesis and biological evaluation of novel dual inhibitors of acetylcholinesterase and beta-secretase.EBI Chinese Academy of Sciences
19013792 37 Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors.EBI University of Illinois at Chicago
19013073 2 Identification of pharmacophore model, synthesis and biological evaluation of N-phenyl-1-arylamide and N-phenylbenzenesulfonamide derivatives as BACE 1 inhibitors.EBI Zhejiang University
18842420 44 Design, synthesis and SAR of potent statine-based BACE-1 inhibitors: exploration of P1 phenoxy and benzyloxy residues.EBI Linköping University
18468890 69 Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors.EBI Schering-Plough Research Institute
18457385 41 Recent developments in fragment-based drug discovery.EBI Astex Therapeutics Ltd.
18334299 6 Tetramic and tetronic acids: an update on new derivatives and biological aspects.EBI University of Bayreuth
18261904 10 Novel non-peptidic and small-sized BACE1 inhibitors.EBI Kyoto Pharmaceutical University
18180160 17 Potent memapsin 2 (beta-secretase) inhibitors: design, synthesis, protein-ligand X-ray structure, and in vivo evaluation.EBI Purdue University
18166458 90 BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character.EBI GlaxoSmithKline R&D
18162398 43 Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets.EBI Wyeth Research
17985862 45 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.EBI AstraZeneca Pharmaceuticals LP
17827011 12 Strategies toward improving the brain penetration of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI Merck Research Laboratories
17761418 16 Thiophene substituted acylguanidines as BACE1 inhibitors.EBI Wyeth Research
17583334 13 Discovery of isonicotinamide derived beta-secretase inhibitors: in vivo reduction of beta-amyloid.EBI TBA
17482814 37 Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors.EBI Merck Research Laboratories
17434734 28 Potent and selective isophthalamide S2 hydroxyethylamine inhibitors of BACE1.EBI Pfizer Global Research and Development
17433698 6 Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1).EBI Technische Universität München
17049233 82 Design of potent inhibitors of human beta-secretase. Part 2.EBI Pfizer Inc.
17046251 38 Design of potent inhibitors of human beta-secretase. Part 1.EBI Pfizer Inc.
16757166 4 beta-Secretase inhibitors: modification at the P4 position and improvement of inhibitory activity in cultured cells.EBI Kyoto Pharmaceutical University
16481167 8 Design and synthesis of potent beta-secretase (BACE1) inhibitors with P1' carboxylic acid bioisosteres.EBI Kyoto Pharmaceutical University
16412632 17 BACE-1 inhibitory activities of new substituted phenyl-piperazine coupled to various heterocycles: chromene, coumarin and quinoline.EBI INSERM
16078830 12 Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations.EBI University of Zürich
15582441 5 Design and synthesis of highly active Alzheimer's beta-secretase (BACE1) inhibitors, KMI-420 and KMI-429, with enhanced chemical stability.EBI Kyoto Pharmaceutical University
15582431 1 Synthesis of digalactosyl diacylglycerols and their structure-inhibitory activity on human lanosterol synthase.EBI National Institute of Health Sciences
15509178 37 Efficient evaluation of binding free energy using continuum electrostatics solvation.EBI University of Zürich
15177452 12 Synthesis and SAR of bis-statine based peptides as BACE 1 inhibitors.EBI Wyeth Research
15006396 4 KMI-358 and KMI-370, highly potent and small-sized BACE1 inhibitors containing phenylnorstatine.EBI Kyoto Pharmaceutical University
14741251 12 Rational design and synthesis of selective BACE-1 inhibitors.EBI Merck Research Laboratories
14643307 1 KMI-008, a novel beta-secretase inhibitor containing a hydroxymethylcarbonyl isostere as a transition-state mimic: design and synthesis of substrate-based octapeptides.EBI Kyoto Pharmaceutical University
14592472 13 Green tea catechins as a BACE1 (beta-secretase) inhibitor.EBI Kyungpook National University
14561080 9 Human beta-secretase (BACE) and BACE inhibitors.EBI Elan Pharmaceuticals
12723942 38 Design and synthesis of statine-based cell-permeable peptidomimetic inhibitors of human beta-secretase.EBI Elan Pharmaceuticals
21222511 23 Design, synthesis and SAR study of hydroxychalcone inhibitors of human ▀-secretase (BACE1).BDB Shanghai Institute of Materia Medica, Chinese Academy of Sciences
27289559 38 Design and synthesis of novel anti-Alzheimer's agents: Acridine-chromenone and quinoline-chromenone hybrids.BDB Tehran University of Medical Sciences
16827559 24 Synthesis of tetramic and tetronic acids as beta-secretase inhibitors.BDB Darmstadt Technical University
22882897 7 Synthesis, in vitro Biological Evaluation and Molecular Docking Studies of Benzimidamides as Potential BACE1 Inhibitors.BDB Peking University Health Science Center
22381116 2 The discovery of novel ╬▓-secretase inhibitors: pharmacophore modeling, virtual screening, and docking studies.BDB Peking University Health Science Center
18760609 66 Achiral oligoamines as versatile tool for the development of aspartic protease inhibitors.BDB Philipps-University Marburg
19406640 58 Second generation of BACE-1 inhibitors part 3: Towards non hydroxyethylamine transition state mimetics.BDB GSK
19477642 87 Second generation of BACE-1 inhibitors part 2: Optimisation of the non-prime side substituent.BDB GSK
19428244 60 Second generation of BACE-1 inhibitors. Part 1: The need for improved pharmacokinetics.BDB GSK
19195886 22 Structure-based design and synthesis of macrocyclic peptidomimetic beta-secretase (BACE-1) inhibitors.BDB Novartis
18171615 69 BACE-1 inhibitors part 3: identification of hydroxy ethylamines (HEAs) with nanomolar potency in cells.BDB GSK
18457381 36 Second generation of hydroxyethylamine BACE-1 inhibitors: optimizing potency and oral bioavailability.BDB GSK
19036583 18 Identification of a small molecule beta-secretase inhibitor that binds without catalytic aspartate engagement.BDB Merck Research Laboratories
18811140 11 Discovery and X-ray crystallographic analysis of a spiropiperidine iminohydantoin inhibitor of beta-secretase.BDB Merck Research Laboratories
17685503 6 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.BDB Johnson & Johnson Pharmaceutical
11520194 13 Structure-based design: potent inhibitors of human brain memapsin 2 (beta-secretase).BDB University of Illinois at Chicago
14695829 21 Design and synthesis of hydroxyethylene-based peptidomimetic inhibitors of human beta-secretase.BDB Elan Pharmaceuticals
17034121 20 Acylguanidines as small-molecule beta-secretase inhibitors.BDB Wyeth Research
16821787 28 Naphthyl and coumarinyl biarylpiperazine derivatives as highly potent human beta-secretase inhibitors. Design, synthesis, and enzymatic BACE-1 and cell assays.BDB Universite de la Mediterranee
17034118 8 Macrocyclic inhibitors of beta-secretase: functional activity in an animal model.BDB Merck Research Laboratories
17107793 12 Evaluating scoring functions for docking and designing beta-secretase inhibitors.BDB Merck Research Laboratories
17112725 3 Beta-secretase (BACE-1) inhibitors: accounting for 10s loop flexibility using rigid active sites.BDB Merck Research Laboratories
16690314 13 BACE-1 inhibition by a series of psi[CH2NH] reduced amide isosteres.BDB Merck Research Laboratories
17257835 15 Discovery and SAR of isonicotinamide BACE-1 inhibitors that bind beta-secretase in a N-terminal 10s-loop down conformation.BDB Merck Research Laboratories
15588077 15 Structure-based design of potent and selective cell-permeable inhibitors of human beta-secretase (BACE-1).BDB Merck Research Laboratories
16451048 7 Aminoethylenes: a tetrahedral intermediate isostere yielding potent inhibitors of the aspartyl protease BACE-1.BDB Sunesis
15582402 9 Structure-based design of cycloamide-urethane-derived novel inhibitors of human brain memapsin 2 (beta-secretase).BDB University of Illinois at Chicago
17432843 22 Design, synthesis, and X-ray structure of potent memapsin 2 (beta-secretase) inhibitors with isophthalamide derivatives as the P2-P3-ligands.BDB Purdue University
16620080 15 Design, synthesis and X-ray structure of protein-ligand complexes: important insight into selectivity of memapsin 2 (beta-secretase) inhibitors.BDB Purdue University
16854060 58 Structure-based design and synthesis of macroheterocyclic peptidomimetic inhibitors of the aspartic protease beta-site amyloid precursor protein cleaving enzyme (BACE).BDB Universite de Montreal at Succursale Centre-Ville
16078837 34 Structure-based design, synthesis, and memapsin 2 (BACE) inhibitory activity of carbocyclic and heterocyclic peptidomimetics.BDB Universite de Montreal at Succursale Centre-Ville
15566281 5 Identification of a small molecule nonpeptide active site beta-secretase inhibitor that displays a nontraditional binding mode for aspartyl proteases.BDB Merck Research Laboratories
17149856 8 Discovery of oxadiazoyl tertiary carbinamine inhibitors of beta-secretase (BACE-1).BDB Merck Research Laboratories
16263281 15 Conformationally biased P3 amide replacements of beta-secretase inhibitors.BDB Merck Research Laboratories
16249081 7 Macrocyclic peptidomimetic inhibitors of beta-secretase (BACE): first X-ray structure of a macrocyclic peptidomimetic-BACE complex.BDB Lilly S.A.
17300163 9 Design, synthesis, and crystal structure of hydroxyethyl secondary amine-based peptidomimetic inhibitors of human beta-secretase.BDB Elan Pharmaceuticals
17315856 5 Application of fragment screening by X-ray crystallography to beta-secretase.BDB Astex
17315857 11 Application of fragment screening by X-ray crystallography to the discovery of aminopyridines as inhibitors of beta-secretase.BDB Astex