Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core

J M Fevig; D J Pinto; Q Han; M L Quan; J R Pruitt; I C Jacobson; R A Galemmo Jr; S Wang; M J Orwat; L L Bostrom; R M Knabb; P C Wong; Lam PYS; R R Wexler

doi:10.1016/s0960-894x(01)00029-4

Synthesis and SAR of benzamidine factor Xa inhibitors containing a vicinally-substituted heterocyclic core

Bioorg Med Chem Lett. 2001 Mar 12;11(5):641-5. doi: 10.1016/s0960-894x(01)00029-4.

Authors

J M Fevig¹, D J Pinto, Q Han, M L Quan, J R Pruitt, I C Jacobson, R A Galemmo Jr, S Wang, M J Orwat, L L Bostrom, R M Knabb, P C Wong, Lam PYS, R R Wexler

Affiliation

¹ DuPont Pharmaceuticals Company, Wilmington, DE 19880-0500, USA. john.m.fevig@dupontpharma.com

PMID: 11266160
DOI: 10.1016/s0960-894x(01)00029-4

Abstract

The selective inhibition of coagulation factor Xa has emerged as an attractive strategy for the discovery of novel antithrombotic agents. Here we describe highly potent benzamidine factor Xa inhibitors based on a vicinally-substituted heterocyclic core.

MeSH terms

Animals
Benzamidines / chemical synthesis
Benzamidines / chemistry*
Benzamidines / pharmacology*
Factor Xa Inhibitors*
Heterocyclic Compounds / chemical synthesis
Heterocyclic Compounds / chemistry*
Humans
Kinetics
Molecular Structure
Rabbits
Serine Proteinase Inhibitors / chemical synthesis
Serine Proteinase Inhibitors / chemistry*
Serine Proteinase Inhibitors / pharmacology
Structure-Activity Relationship

Substances

Benzamidines
Factor Xa Inhibitors
Heterocyclic Compounds
Serine Proteinase Inhibitors