Thrombin active site inhibitors: Chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues

Jagabandhu Das, S. David Kimball, Joyce A. Reid, Tammy C. Wang, Wan F. Lau, Daniel G.M. Roberts, Steven M. Seiler, William A. Schumacher, Martin L. Ogletree

Research output: Contribution to journalArticle

14 Scopus citations

Abstract

A series of structurally novel small molecule inhibitors of human α-thrombin was prepared to elucidate their structure- activity relationships (SAR), selectivity and activity in vivo. BMS-189090 (5) is identified as a potent, selective, and reversible inhibitor of human α-thrombin that is efficacious in vivo in a mice lethality model, and in inhibiting both arterial and venous thrombosis in a rat model.

Original languageEnglish (US)
Pages (from-to)41-44
Number of pages4
JournalBioorganic and Medicinal Chemistry Letters
Volume12
Issue number1
DOIs
StatePublished - Jan 7 2002
Externally publishedYes

All Science Journal Classification (ASJC) codes

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

Fingerprint Dive into the research topics of 'Thrombin active site inhibitors: Chemical synthesis, in vitro and in vivo pharmacological profile of a novel and selective agent BMS-189090 and analogues'. Together they form a unique fingerprint.

  • Cite this