The following articles (labelled with PubMed ID or TBD) are for your review
| PMID | Data | Article Title | Organization |
|---|
| 26608551 |
35 |
Synthesis of (3S,4S)-4-aminopyrrolidine-3-ol derivatives and biological evaluation for their BACE1 inhibitory activities. |
Korea University of Science and Technology |
| 26061085 |
13 |
Peptidomimeticß-Secretase Inhibitors Comprising a Sequence of Amyloid-ß Peptide for Alzheimer's Disease. |
Instituto De Biologia Experimental E Tecnol£Gica |
| 26001341 |
19 |
Preparation and biological evaluation of conformationally constrained BACE1 inhibitors. |
Eli Lilly |
| 25782742 |
76 |
trans-(3S,4S)-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part I: prime site exploration using an amino linker. |
Novartis Pharma |
| 25754490 |
44 |
trans-3,4-Disubstituted pyrrolidines as inhibitors of the human aspartyl protease renin. Part II: prime site exploration using an oxygen linker. |
Novartis Pharma |
| 25728416 |
25 |
Iminopyrimidinones: a novel pharmacophore for the development of orally active renin inhibitors. |
Merck Research Laboratories |
| 25050166 |
58 |
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors. |
Novartis Institutes For Biomedical Research |
| 25537272 |
17 |
Structure-based design, synthesis and biological evaluation of novelß-secretase inhibitors containing a pyrazole or thiazole moiety as the P3 ligand. |
Purdue University |
| 25363711 |
62 |
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 |
| 24704031 |
69 |
The evolution of amidine-based brain penetrant BACE1 inhibitors. |
Janssen Pharmaceutica |
| 23590342 |
105 |
ß-Secretase (BACE1) inhibitors with high in vivo efficacy suitable for clinical evaluation in Alzheimer's disease. |
F. Hoffmann-La Roche |
| 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. |
Novartis Pharma |
| 23374014 |
24 |
Discovery of biphenylacetamide-derived inhibitors of BACE1 using de novo structure-based molecular design. |
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. |
Novartis Pharma |
| 23017051 |
69 |
New aminoimidazoles asß-secretase (BACE-1) inhibitors showing amyloid-ß (Aß) lowering in brain. |
Astrazeneca |
| 22954357 |
29 |
Structure-based design of highly selectiveß-secretase inhibitors: synthesis, biological evaluation, and protein-ligand X-ray crystal structure. |
Purdue University |
| 22924815 |
97 |
Design and synthesis ofß-site amyloid precursor protein cleaving enzyme (BACE1) inhibitors with in vivo brain reduction ofß-amyloid peptides. |
Astrazeneca |
| 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. |
Medivir |
| 23412139 |
26 |
Discovery of an Orally Available, Brain Penetrant BACE1 Inhibitor that Affords Robust CNS Aß Reduction. |
TBA |
| 22390835 |
80 |
Structure based design of iminohydantoin BACE1 inhibitors: identification of an orally available, centrally active BACE1 inhibitor. |
Merck Research Laboratories |
| 20579874 |
150 |
BACE-1 hydroxyethylamine inhibitors using novel edge-to-face interaction with Arg-296. |
Glaxosmithkline |
| 20045648 |
39 |
Di-substituted pyridinyl aminohydantoins as potent and highly selective human beta-secretase (BACE1) inhibitors. |
Wyeth Research |
| 17980584 |
72 |
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor. |
Schering-Plough Research Institute |
| 18171614 |
63 |
BACE-1 inhibitors part 1: identification of novel hydroxy ethylamines (HEAs). |
Glaxosmithkline |
| 18023580 |
50 |
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors. |
Schering-Plough Research Institute |
| 11405641 |
8 |
Secretase targets for Alzheimer's disease: identification and therapeutic potential. |
Harvard Medical School |
| 14684335 |
21 |
Phe*-Ala-based pentapeptide mimetics are BACE inhibitors: P2 and P3 SAR. |
Eli Lilly |
| 22130130 |
19 |
Discovery of pyrrolidine-basedß-secretase inhibitors: lead advancement through conformational design for maintenance of ligand binding efficiency. |
Merck Research Laboratories |
| 22044119 |
84 |
Design, synthesis, and qualitative structure-activity evaluations of novelß-secretase inhibitors as potential Alzheimer's drug leads. |
University of Sharjah |
| 21835615 |
165 |
New pyrazolyl and thienyl aminohydantoins as potent BACE1 inhibitors: exploring the S2' region. |
Pfizer |
| 20880704 |
200 |
Design and synthesis of aminohydantoins as potent and selective humanß-secretase (BACE1) inhibitors with enhanced brain permeability. |
Pfizer |
| 20656487 |
45 |
Fragment-based discovery and optimization of BACE1 inhibitors. |
Evotec |
| 20347593 |
76 |
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization. |
Merck Research Laboratories |
| 20223661 |
48 |
Novel pyrrolyl 2-aminopyridines as potent and selective human beta-secretase (BACE1) inhibitors. |
Wyeth |
| 20202842 |
47 |
Pyridinyl aminohydantoins as small molecule BACE1 inhibitors. |
Wyeth Research |
| 20172717 |
35 |
Structure-based design and synthesis of novel P2/P3 modified, non-peptidic beta-secretase (BACE-1) inhibitors. |
Universit£ |
| 19959359 |
46 |
Discovery and initial optimization of 5,5'-disubstituted aminohydantoins as potent beta-secretase (BACE1) inhibitors. |
Wyeth Research |
| 19968289 |
201 |
Design and synthesis of 5,5'-disubstituted aminohydantoins as potent and selective human beta-secretase (BACE1) inhibitors. |
Wyeth Research |
| 19757823 |
98 |
Aminoimidazoles as potent and selective human beta-secretase (BACE1) inhibitors. |
Wyeth Research |
| 19323561 |
11 |
Harnessing nature's insight: design of aspartyl protease inhibitors from treatment of drug-resistant HIV to Alzheimer's disease. |
Purdue University |
| 19013792 |
37 |
Molecular modeling, synthesis, and activity studies of novel biaryl and fused-ring BACE1 inhibitors. |
University of Illinois At Chicago |
| 18468890 |
69 |
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors. |
Schering-Plough Research Institute |
| 18166458 |
90 |
BACE-1 inhibitors part 2: identification of hydroxy ethylamines (HEAs) with reduced peptidic character. |
Glaxosmithkline |
| 18162398 |
43 |
Acylguanidine inhibitors of beta-secretase: optimization of the pyrrole ring substituents extending into the S1 and S3 substrate binding pockets. |
Wyeth Research |
| 17482814 |
37 |
Design, synthesis, and SAR of macrocyclic tertiary carbinamine BACE-1 inhibitors. |
Merck Research Laboratories |
| 17433698 |
6 |
Synthesis and biological evaluation of phosphino dipeptide isostere inhibitor of human beta-secretase (BACE1). |
Technische UniversitäT MüNchen |
| 16078830 |
12 |
Discovery of cell-permeable non-peptide inhibitors of beta-secretase by high-throughput docking and continuum electrostatics calculations. |
University of ZüRich |
| 28427814 |
24 |
Design, synthesis, and X-ray structural studies of BACE-1 inhibitors containing substituted 2-oxopiperazines as P1'-P2' ligands. |
Purdue University |
| 9225287 |
174 |
RS-102221: a novel high affinity and selective, 5-HT2C receptor antagonist. |
Roche Bioscience |
| 9223586 |
8 |
[125I]IPH, an epibatidine analog, binds with high affinity to neuronal nicotinic cholinergic receptors. |
Georgetown University |
| 9223553 |
16 |
[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 |
| 7616392 |
5 |
Functional characterization of the nonpeptide neurokinin3 (NK3) receptor antagonist, SR142801 on the human NK3 receptor expressed in Chinese hamster ovary cells. |
Sanofi Recherche |
| 6325601 |
52 |
Cholecystokinin receptors: biochemical demonstration and autoradiographical localization in rat brain and pancreas using [3H] cholecystokinin8 as radioligand. |
F. Hoffmann-La Roche |
| 18785742 |
18 |
A novel class of small molecule inhibitors of Hsp90. |
Yale University |
| 18835174 |
17 |
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 |
| 12773033 |
17 |
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 |
| 17004721 |
49 |
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 |
| 16033281 |
19 |
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 |
| 15239657 |
30 |
Novel azapeptide inhibitors of hepatitis C virus serine protease. |
Boehringer Ingelheim (Canada) |
| 12699382 |
4 |
An ethylenamine inhibitor binds tightly to both wild type and mutant HIV-1 proteases. Structure and energy study. |
Academy of Sciences of The Czech Republic |
Search and Browse
