1,2-Disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors

K Takeuchi; J A Bastian; D S Gifford-Moore; R W Harper; S C Miller; J T Mullaney; D J Sall; G F Smith; M Zhang; M J Fisher

doi:10.1016/s0960-894x(00)00454-6

1,2-Disubstituted indole, azaindole and benzimidazole derivatives possessing amine moiety: a novel series of thrombin inhibitors

Bioorg Med Chem Lett. 2000 Oct 16;10(20):2347-51. doi: 10.1016/s0960-894x(00)00454-6.

Authors

K Takeuchi¹, J A Bastian, D S Gifford-Moore, R W Harper, S C Miller, J T Mullaney, D J Sall, G F Smith, M Zhang, M J Fisher

Affiliation

¹ Lilly Research Laboratories, Eli Lilly and Company, Lilly Corporate Center, Indianapolis, IN 46285, USA. ktak@lilly.com

PMID: 11055353
DOI: 10.1016/s0960-894x(00)00454-6

Abstract

A novel series of 1,2-disubstituted indole, azaindole and benzimidazole derivatives possessing an amine moiety was identified as thrombin inhibitors. An indole with basic diamine moieties (12a) was the most potent thrombin inhibitor in the series with Kass= 197 x 10(6) L/mol.

MeSH terms

Amines / chemical synthesis
Amines / chemistry
Amines / pharmacology
Anticoagulants / chemical synthesis*
Anticoagulants / chemistry
Anticoagulants / pharmacology
Aza Compounds / chemical synthesis*
Aza Compounds / chemistry
Aza Compounds / pharmacology
Benzimidazoles / chemical synthesis*
Benzimidazoles / chemistry
Benzimidazoles / pharmacology
Drug Design
Indoles / chemical synthesis*
Indoles / chemistry
Indoles / pharmacology
Kinetics
Molecular Structure
Structure-Activity Relationship
Thrombin / antagonists & inhibitors*

Substances

Amines
Anticoagulants
Aza Compounds
Benzimidazoles
Indoles
Thrombin