2. Academic Validation
  3. Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664

Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin active site inhibitor BMS-189664

  • Bioorg Med Chem Lett. 2002 Jan 7;12(1):45-9. doi: 10.1016/s0960-894x(01)00667-9.
Jagabandhu Das 1,  S David Kimball,  Steven E Hall,  Wen Ching Han,  Edwin Iwanowicz,  James Lin,  Robert V Moquin,  Joyce A Reid,  John S Sack,  Mary F Malley,  Chiehying Y Chang,  Saeho Chong,  David B Wang-Iverson,  Daniel G M Roberts,  Steven M Seiler,  William A Schumacher,  Martin L Ogletree
Affiliations

Affiliation

  • 1 Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. jagabandhu.das@bms.com
PMID: 11738570 DOI: 10.1016/s0960-894x(01)00667-9
Abstract

A series of structurally novel small molecule inhibitors of human alpha-thrombin was prepared to elucidate their structure-activity relationships (SARs), selectivity and activity in vivo. BMS-189664 (3) is identified as a potent, selective, and orally active reversible inhibitor of human alpha-thrombin which is efficacious in vivo in a mouse lethality model, and at inhibiting both arterial and venous thrombosis in cynomolgus monkey models.

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