The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27690432 |
75 |
Discovery of Second Generation Reversible Covalent DPP1 Inhibitors Leading to an Oxazepane Amidoacetonitrile Based Clinical Candidate (AZD7986). |
Charles River Discovery Research Services |
27211244 |
9 |
Tasiamide F, a potent inhibitor of cathepsins D and E from a marine cyanobacterium. |
University of Florida |
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 |
25086681 |
57 |
Structure-based optimization of non-peptidic Cathepsin D inhibitors. |
Merck |
25050166 |
58 |
Structure-based design of substituted piperidines as a new class of highly efficacious oral direct Renin inhibitors. |
Novartis Institutes For Biomedical Research |
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). |
Amgen |
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 |
23360239 |
19 |
A novel class of oral direct renin inhibitors: highly potent 3,5-disubstituted piperidines bearing a tricyclic p3-p1 pharmacophore. |
Novartis Pharma |
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. |
University of Florida |
24900544 |
8 |
Discovery of DS-8108b, a Novel Orally Bioavailable Renin Inhibitor. |
TBA |
22748705 |
2 |
Total synthesis of grassystatin A, a probe for cathepsin E function. |
Fudan University |
22360587 |
1 |
Symplocin A, a linear peptide from the Bahamian cyanobacterium Symploca sp. Configurational analysis of N,N-dimethylamino acids by chiral-phase HPLC of naphthacyl esters. |
University of California |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University of Florida |
17980584 |
72 |
Discovery of an orally efficaceous 4-phenoxypyrrolidine-based BACE-1 inhibitor. |
Schering-Plough Research Institute |
18023580 |
50 |
Potent pyrrolidine- and piperidine-based BACE-1 inhibitors. |
Schering-Plough Research Institute |
2002469 |
80 |
Renin inhibitors containing conformationally restricted P1-P1' dipeptide mimetics. |
Merck Sharp and Dohme Research Laboratories |
| 37 |
Peptidomimetic inhibitors of human immunodeficiency virus protease (HIV-PR): Design, enzyme binding and selectivity, antiviral efficacy, and cell permeability properties |
TBA |
20731374 |
65 |
Direct renin inhibitors as a new therapy for hypertension. |
Novartis Pharmaceuticals |
20347593 |
76 |
Piperazine sulfonamide BACE1 inhibitors: design, synthesis, and in vivo characterization. |
Merck Research Laboratories |
20102207 |
7 |
Synthesis and preclinical evaluations of 2-(2-fluorophenyl)-6,7-methylenedioxyquinolin-4-one monosodium phosphate (CHM-1-P-Na) as a potent antitumor agent. |
China Medical University |
19963375 |
30 |
Macrocyclic BACE-1 inhibitors acutely reduce Abeta in brain after po application. |
Novartis Institutes For Biomedical Research |
| 22 |
Novel pseudosymmetric inhibitors of HIV-1 protease |
TBA |
18468890 |
69 |
Rational design of novel, potent piperazinone and imidazolidinone BACE1 inhibitors. |
Schering-Plough Research Institute |
31913032 |
86 |
Plasmepsin Inhibitors in Antimalarial Drug Discovery: Medicinal Chemistry and Target Validation (2000 to Present). |
University of Zambia |
31589043 |
91 |
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 |
8410992 |
35 |
Renin inhibitors containing a pyridyl amino diol derived C-terminus. |
Hoechst |
8410973 |
75 |
Specificity in the binding of inhibitors to the active site of human/primate aspartic proteinases: analysis of P2-P1-P1'-P2' variation. |
University of Florida |
29087712 |
34 |
Grassystatins D-F, Potent Aspartic Protease Inhibitors from Marine Cyanobacteria as Potential Antimetastatic Agents Targeting Invasive Breast Cancer. |
University of Florida |