New advances in the discovery of thrombin and factor Xa inhibitors

Current Opinion in Chemical Biology

Volumn 4, Issue 4, 2000, Pages 394-400

  Vacca, Joseph P ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

2 (3 CARBAMIMIDOYL BENZYL) 3 [(3',4'DIMETHOXY BIPHENYL 4 CARBONYL)AMINO] BUTYRIC ACID METHYL ESTER TRIFLUOROACETIC ACID; ACETYL DEXTRO PHENYLALANYLPROLYLBOROARGININE; ANILINE; ANTITHROMBOCYTIC AGENT; ARGATROBAN; BLOOD CLOTTING FACTOR 10A; BLOOD CLOTTING FACTOR 10A INHIBITOR; BLOOD CLOTTING FACTOR 13; BLOOD CLOTTING FACTOR 5; BLOOD CLOTTING FACTOR 8; FIBRINOGEN; HEPARIN; HIRUDIN; HIRULOG; LOW MOLECULAR WEIGHT HEPARIN; PIPERIDINE DERIVATIVE; THROMBIN; THROMBIN INHIBITOR; THROMBIN RECEPTOR; UNCLASSIFIED DRUG; WARFARIN;

CHEMICAL MODIFICATION; DEEP VEIN THROMBOSIS; DRUG ABSORPTION; DRUG BIOAVAILABILITY; DRUG DESIGN; DRUG INHIBITION; DRUG MECHANISM; DRUG POTENCY; DRUG RESEARCH; DRUG STRUCTURE; DRUG SYNTHESIS; HEART INFARCTION; NONHUMAN; PATIENT MONITORING; REVIEW; STROKE; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

EID: 0033859659     PISSN: 13675931     EISSN: None     Source Type: Journal    
DOI: 10.1016/S1367-5931(00)00112-5     Document Type: Review

References (39)

1. Strategies and progress towards the ideal orally active thrombin inhibitor
2. Direct thrombin inhibitors
3. Clinical status of direct thrombin inhibitors
4. 7-Azabicycloheptane carboxylic acid: A proline replacement in a boroarginine thrombin inhibitor
5. Design, synthesis and biological evaluation of selective boron-containing thrombin inhibitors
6. Potent and selective bicyclic lactam inhibitors of thrombin. Part 3: P1' modifications
7. Structural basis of the thrombin selectivity of a ligand that contains the constrained arginine mimic (2S)-2-Amino-(3S)-3-(1-carbamimidoyl-piperidin-3-yl)-propanoic acid at P1
8. Secondary structure peptide mimetics: Design, synthesis, and evaluation of β-strand mimetic thrombin inhibitors
9. Investigation of the S3 site of thrombin: Design, synthesis and biological activity of 4-substituted 3-amino-2-pyridones incorporating P1-argininals
10. Crystal structures of thrombin complexed to a novel series of synthetic inhibitors containing a 5,5-trans-lactone template
11. Exploring the chiral space within the active site of α-thrombin with a constrained mimic of D-Phe-Pro-Arg - Design, synthesis, inhibitory activity, and X-ray structure of an enzyme-inhibitor complex
12. Structure-based design and synthesis of novel thrombin inhibitors based on phosphinic peptide mimetics
13. 1-Aminoisoquinoline as benzamidine isoster in the design and synthesis of orally active thrombin inhibitors
14. Protease inhibitors - part 3. Synthesis of non-basic thrombin inhibitors incorporating pyridinium-sulfanilylguanidine moieties at the P1 site
15. Studies towards the identification of potent, selective and bioavailable thrombin inhibitors
16. Optimisation of the P2 pharmacophore in a series of thrombin inhibitors: Ion-dipole interactions with lysine 60G
17. Fluorobenzamidrazone thrombin inhibitors: Influence of fluorine on enhancing oral absorption
18. The design of potent, selective non-covalent, peptide thrombin inhibitors utilizing Imidazole as a S1 binding element
19. Structure-activity and crystallographic analysis of a new class of non-amide-based thrombin inhibitor
20. Amidinohydrazones as guanidine bioisosteres: Application to a new class of potent, selective and orally bioavailable, non-amide-based small-molecule thrombin inhibitors
21. Non-peptidic phenyl-based thrombin inhibitors: Exploring structural requirements of the S1 specificity pocket with amidines
22. Combinatorial docking and combinatorial chemistry: Design of potent non-peptide thrombin inhibitors
23. Design and synthesis of potent and selective 5,6-fused heterocyclic thrombin inhibitors
24. Diamino Benzo[b]thiophene derivatives as a novel class of active site directed thrombin inhibitors. 5. Potency, efficacy, and pharmacokinetic properties of modified C-3 side chain derivatives
25. Dibasic benzo[B]thiophene derivatives as a novel class of active site directed thrombin inhibitors: 4. SAR studies on the conformationally restricted C3-side chain of hydroxybenzo[B]thiophenes
26. Progress in the design of inhibitors of coagulation factor Xa
27. Design, synthesis and structure-activity relationship of a series of arginine aldehyde factor Xa inhibitors. Part 1: Structures based on the (D)-Arg-Gly-Arg tripeptide sequence
28. Guanylpiperidine peptidomimetics: Potent and selective biscation inhibitors of factor Xa
29. Synthesis, characterization, and structure-activity relationships of amidine-substituted (bis)benzylidene-cycloketone olefin isomers as potent and selective factor Xa inhibitors
30. The de novo design and synthesis of cyclic urea inhibitors of factor Xa: Optimization of the S4 ligand
31. Amido-(propyl and allyl)-hydroxybenzamidines: Development of achiral inhibitors of Factor Xa
32. Isoxazolines and isoxazoles as factor Xa inhibitors
33. Nonpeptide factor Xa inhibitors: 1. Studies with SF303 and SK549, a new class of potent antithrombotics
34. N2-aroylanthranilamide inhibitors of human factor Xa
35. 1,2-Dibenzamidobenzene inhibitors of human factor Xa
36. Structure-based design of potent, amidine-derived inhibitors of factor Xa: Evaluation of selectivity, anticoagulant activity, and antithrombotic activity
37. Design, synthesis, and in vitro biological activity of indole-based factor Xa inhibitors
38. Design, synthesis, and in vitro biological activity of benzimidazole based factor Xa inhibitors
39. Antithrombotic efficacy of RPR208566, a novel factor Xa inhibitor, in a rat model of carotid artery thrombosis