5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa

Jennifer X Qiao; Xuhong Cheng; Dilip P Modi; Karen A Rossi; Joseph M Luettgen; Robert M Knabb; Prabhakar K Jadhav; Ruth R Wexler

doi:10.1016/j.bmcl.2004.10.045

5-Amidinobenzo[b]thiophenes as dual inhibitors of factors IXa and Xa

Bioorg Med Chem Lett. 2005 Jan 3;15(1):29-35. doi: 10.1016/j.bmcl.2004.10.045.

Authors

Jennifer X Qiao¹, Xuhong Cheng, Dilip P Modi, Karen A Rossi, Joseph M Luettgen, Robert M Knabb, Prabhakar K Jadhav, Ruth R Wexler

Affiliation

¹ Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 5400, Princeton, NJ 08543-5400, USA. [email protected]

PMID: 15582405
DOI: 10.1016/j.bmcl.2004.10.045

Abstract

Syntheses and SAR studies of 5-amidinobenzo[b]thiophene analogs provided compounds with low submicromolar factor IXa activity and equal or slightly better selectivity relative to factor Xa.

MeSH terms

Factor IXa / antagonists & inhibitors*
Factor Xa Inhibitors*
Serine Proteinase Inhibitors / chemistry
Serine Proteinase Inhibitors / pharmacology*
Structure-Activity Relationship
Thiophenes / chemistry
Thiophenes / pharmacology*

Substances

Factor Xa Inhibitors
Serine Proteinase Inhibitors
Thiophenes
Factor IXa