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Molecular design and structure--activity relationships leading to the potent, selective, and orally active thrombin
Jagabandhu Das1, S David Kimball, Steven E Hall
1Bristol-Myers Squibb Pharmaceutical Research Institute, Princeton, NJ 08543-4000, USA. jagabandhu.das@bms.com
Bioorganic & Medicinal Chemistry Letters
|December 12, 2001
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.