The following articles (labelled with PubMed ID or TBD) are for your review
PMID | Data | Article Title | Organization |
27977181 |
8 |
An Orally Active Bradykinin B |
Nanyang Technological University |
1433218 |
3 |
Guanidinophenyl-substituted enol lactones as selective, mechanism-based inhibitors of trypsin-like serine proteases. |
University Of Illinois |
19715320 |
87 |
Grassystatins A-C from marine cyanobacteria, potent cathepsin E inhibitors that reduce antigen presentation. |
University Of Florida |
15837303 |
52 |
Solid-phase synthesis of naphthylamidines as factor VIIa/tissue factor inhibitors. |
Berlex Biosciences |
12904065 |
30 |
Efficacious and orally bioavailable thrombin inhibitors based on a 2,5-thienylamidine at the P1 position: discovery of N-carboxymethyl-d-diphenylalanyl-l-prolyl[(5-amidino-2-thienyl)methyl]amide. |
Lg Life Sciences |
10956211 |
14 |
GRID/CPCA: a new computational tool to design selective ligands. |
Boehringer Ingelheim Pharma |
8759623 |
31 |
Potent thrombin inhibitors that probe the S1 subsite: tripeptide transition state analogues based on a heterocycle-activated carbonyl group. |
R. W. Johnson Pharmaceutical Research Institute |
7966150 |
60 |
Design and synthesis of potent and highly selective thrombin inhibitors. |
F. Hoffmann-La Roche |
8478905 |
53 |
Inhibition studies of some serine and thiol proteinases by new leupeptin analogues. |
University Of Arkansas |
8496923 |
9 |
New mechanism-based inactivators of trypsin-like proteinases. Selective inactivation of urokinase by functionalized cyclopeptides incorporating a sulfoniomethyl-substituted m-aminobenzoic acid residue. |
Cnrs-Cercoa |
2231595 |
96 |
Selective inhibition of urokinase by substituted phenylguanidines: quantitative structure-activity relationship analyses. |
Abbott Laboratories |
15081015 |
91 |
Solid-phase synthesis and SAR of 4-carboxy-2-azetidinone mechanism-based tryptase inhibitors. |
The Bristol-Myers Squibb Pharmaceutical Research Institute |
12781189 |
6 |
D-Phe-Pro-Arg type thrombin inhibitors: unexpected selectivity by modification of the P1 moiety. |
Basf |
11909707 |
69 |
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1. |
Life Science R & D, Lgci |
11459667 |
13 |
Selectivity enhancement induced by substitution of non-natural analogues of arginine and lysine in arginine-based thrombin inhibitors. |
Medical University Of South Carolina |
| 34 |
Peptidyl -keto thiazole as potent thrombin inhibitors |
TBA |
| 22 |
Design and synthesis of conformationally constrained arginal thrombin inhibitors |
TBA |
| 48 |
DERIVATIVES OF 4-AMINO-PYRIDINE AS SELECTIVE THROMBIN INHIBITORS |
TBA |
| 19 |
Rational design of selective thrombin inhibitors |
TBA |
| 37 |
Synthesis and biological activity of P2–P4 azapeptidomimetic P1-argininal and P1-ketoargininamide derivatives: a novel class of serine protease inhibitors |
TBA |
| 4 |
Synthesis, evaluation, and crystallographic analysis of L-371,912: A potent and selective active-site thrombin inhibitor |
TBA |
| 24 |
Novel thrombin inhibitors that are based on a macrocyclic tripeptide motif |
TBA |
| 2 |
Kinetic characterization of a peptide inhibitor of trypsin isolated from a synthetic peptide combinatorial library |
TBA |
| 9 |
Diphenylborinic acid is a strong inhibitor of serine proteases |
TBA |
| 13 |
Characterization of LY806303 as a potent and selective inhibitor of thrombin |
TBA |
12951087 |
23 |
Selective 3-amino-2-pyridinone acetamide thrombin inhibitors incorporating weakly basic partially saturated heterobicyclic P1-arginine mimetics. |
University Of Ljubljana |
12372529 |
21 |
Retro-binding thrombin active site inhibitors: identification of an orally active inhibitor of thrombin catalytic activity. |
Bristol-Myers Squibb Pharmaceutical Research Institute |
12372525 |
2 |
A mechanism-based probe for gp120-Hydrolyzing antibodies. |
University Of Texas-Houston Medical School |
11965377 |
66 |
Design and synthesis of aminophenol-based factor Xa inhibitors. |
Berlex Biosciences |
11881991 |
21 |
PRO_SELECT: combining structure-based drug design and array-based chemistry for rapid lead discovery. 2. The development of a series of highly potent and selective factor Xa inhibitors. |
Protherics Molecular Design |
11425539 |
23 |
Inhibition of serine proteases: activity of 1,3-diazetidine-2,4-diones. |
Shionogi |
11133089 |
28 |
Noncovalent thrombin inhibitors incorporating an imidazolylethynyl P1. |
Lg Chemical |
11078187 |
36 |
Synthesis and structure-activity relationships of a new class of 1-oxacephem-based human chymase inhibitors. |
Shionogi |
10853669 |
102 |
Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors. |
Berlex Biosciences |
10782664 |
42 |
Isoxazolines and isoxazoles as factor Xa inhibitors. |
Dupont Pharmaceuticals |
10639283 |
135 |
Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors. |
Berlex Biosciences |
10636250 |
20 |
Non-peptidic phenyl-based thrombin inhibitors: exploring structural requirements of the S1 specificity pocket with amidines. |
3-Dimensional Pharmaceuticals |
10636229 |
27 |
Amidinohydrazones as guanidine bioisosteres: application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors. |
3-Dimensional Pharmaceuticals |
10560742 |
85 |
3-Amidinophenylalanine-based inhibitors of urokinase. |
UniversitäT Jena |
10508439 |
4 |
Conformations of trypsin-bound amidine inhibitors of blood coagulant factor Xa by double REDOR NMR and MD simulations. |
Washington University |
10498193 |
22 |
Fluorobenzamidrazone thrombin inhibitors: influence of fluorine on enhancing oral absorption. |
Biotech Research Institute |
10346927 |
114 |
Design, synthesis, and activity of 2,6-diphenoxypyridine-derived factor Xa inhibitors. |
Berlex Biosciences |
10230630 |
36 |
Thrombin inhibitors based on a propargylglycine template. |
Biotech Research Institute |
10212122 |
35 |
Secondary structure peptide mimetics: design, synthesis, and evaluation of beta-strand mimetic thrombin inhibitors. |
Molecumetics |
9934479 |
17 |
Novel acylguanidine containing thrombin inhibitors with reduced basicity at the P1 moiety. |
Nv Organon Scientific Development Group |
9925737 |
57 |
N-[2,2-dimethyl-3-(N-(4-cyanobenzoyl)amino)nonanoyl]-L-phenylalanine ethyl ester as a stable ester-type inhibitor of chymotrypsin-like serine proteases: structural requirements for potent inhibition of alpha-chymotrypsin. |
Nippon Steel |
9876114 |
111 |
Structural and functional analyses of benzamidine-based inhibitors in complex with trypsin: implications for the inhibition of factor Xa, tPA, and urokinase. |
Institut FüR Biochemie |
9873581 |
21 |
Benzylamine-based selective and orally bioavailable inhibitors of thrombin. |
Biotech Research Institute |
9873520 |
27 |
Design, synthesis, and biological activity of novel purine and bicyclic pyrimidine factor Xa inhibitors. |
Berlex Biosciences |
9873414 |
13 |
Potent and efficacious thienylamidine-incorporated thrombin inhibitors. |
Biotech Research Institute |
9733491 |
21 |
Rational design, synthesis, and X-ray structure of selective noncovalent thrombin inhibitors. |
Novartis Pharma |
9733480 |
93 |
Discovery of N-[2-[5-[Amino(imino)methyl]-2-hydroxyphenoxy]-3, 5-difluoro-6-[3-(4, 5-dihydro-1-methyl-1H-imidazol-2-yl)phenoxy]pyridin-4-yl]-N-methylgl y cine (ZK-807834): a potent, selective, and orally active inhibitor of the blood coagulation enzyme factor Xa. |
Berlex Biosciences |
9733479 |
18 |
(Z,Z)-2,7-Bis(4-amidinobenzylidene)cycloheptan-1-one: identification of a highly active inhibitor of blood coagulation factor Xa. |
Berlex Biosciences |
9544206 |
94 |
2-amino-4H-3,1-benzoxazin-4-ones as inhibitors of C1r serine protease. |
Warner-Lambert |
9406602 |
7 |
Assessment of solvation effects on calculated binding affinity differences: trypsin inhibition by flavonoids as a model system for congeneric series. |
Universidad De Alcalá |
9371237 |
69 |
Discovery of a novel, selective, and orally bioavailable class of thrombin inhibitors incorporating aminopyridyl moieties at the P1 position. |
Merck Research Laboratories |
7739010 |
118 |
Characterization of a class of peptide boronates with neutral P1 side chains as highly selective inhibitors of thrombin. |
Thrombosis Research Institute |
7473571 |
90 |
Structure-activity study of tripeptide thrombin inhibitors using alpha-alkyl amino acids and other conformationally constrained amino acid substitutions. |
Eli Lilly |
6219223 |
94 |
Aromatic amidines: comparison of their ability to block respiratory syncytial virus induced cell fusion and to inhibit plasmin, urokinase, thrombin, and trypsin. |
TBA |
2391691 |
55 |
Inhibition of human leukocyte elastase. 1. Inhibition by C-7-substituted cephalosporin tert-butyl esters. |
Merck Sharp And Dohme Research Laboratories |
1447734 |
29 |
Effect of conformational mobility and hydrogen-bonding interactions on the selectivity of some guanidinoaryl-substituted mechanism-based inhibitors of trypsin-like serine proteases. |
University Of Illinois |
10869410 |
62 |
S33084, a novel, potent, selective, and competitive antagonist at dopamine D(3)-receptors: I. Receptorial, electrophysiological and neurochemical profile compared with GR218,231 and L741,626. |
Centre De Recherches De Croissy |
9802391 |
31 |
The cloned guinea pig pancreatic polypeptide receptor Y4 resembles more the human Y4 than does the rat Y4. |
Uppsala University |
9195867 |
15 |
Structure-based design and combinatorial chemistry yield low nanomolar inhibitors of cathepsin D. |
University Of California Berkeley |
20383151 |
2 |
Small-molecule kinase inhibitors provide insight into Mps1 cell cycle function. |
Dana-Farber Cancer Institute |
19648931 |
16 |
Design, synthesis and selection of DNA-encoded small-molecule libraries. |
Praecis Pharmaceuticals |
19305397 |
22 |
Molecular docking and ligand specificity in fragment-based inhibitor discovery. |
University Of California San Francisco |
| 28 |
A Thermodynamic Study of the Reactions of Cyclodextrins with Primary and Secondary Aliphatic Alcohols, with D- and L-Phenylalanine, and with L-Phenylalanine Amide |
Nist |
19699645 |
12 |
Design, synthesis, and biological evaluation of hydroquinone derivatives as novel inhibitors of the sarco/endoplasmic reticulum calcium ATPase. |
Northern Kentucky University |
17184135 |
28 |
HIV-1 reverse transcriptase structure with RNase H inhibitor dihydroxy benzoyl naphthyl hydrazone bound at a novel site. |
Rutgers University |
14761195 |
114 |
Structural basis for the synthesis of indirubins as potent and selective inhibitors of glycogen synthase kinase-3 and cyclin-dependent kinases. |
University Of Athens |
10531324 |
22 |
Thermodynamic analyses reveal role of water release in epitope recognition by a monoclonal antibody against the human guanylyl cyclase C receptor. |
Indian Institute Of Science |