Format

Send to

Choose Destination
Bioorg Med Chem Lett. 2008 Apr 1;18(7):2428-33. doi: 10.1016/j.bmcl.2008.02.054. Epub 2008 Feb 26.

Sulfonamidolactam inhibitors of coagulation factor Xa.

Author information

1
Bristol-Myers Squibb Company, Cardiovascular Diseases Chemistry, PO Box 5400, Princeton, NJ 08543-5400, USA. joanne.smallheer@bms.com

Abstract

As part of an effort to identify novel backups for previously reported pyrazole-based coagulation Factor Xa inhibitors, the pyrazole 5-carboxamide moiety was replaced by 3-(sulfonylamino)-2-piperidone. This led to the identification of a structurally diverse chemotype that was further optimized to incorporate neutral or weakly basic aryl and heteroaryl P1 groups while maintaining good potency versus Factor Xa. Substitution at the sulfonamide nitrogen provided further improvements in potency and as did introduction of alternate P4 moieties.

PMID:
18329876
DOI:
10.1016/j.bmcl.2008.02.054
[Indexed for MEDLINE]

Supplemental Content

Full text links

Icon for Elsevier Science
Loading ...
Support Center