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

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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Das J,Kimball SD,Hall SE,Han WC,Iwanowicz E,Lin J,Moquin RV,Reid JA,Sack JS,Malley MF,Chang CY,Chong S,Wang-Iverson DB,Roberts DG,Seiler SM,Schumacher WA,Ogletree ML

doi

10.1016/s0960-894x(01)00667-9

subject

Has Abstract

pub_date

2002-01-07 00:00:00

pages

45-9

issue

1

eissn

0960-894X

issn

1464-3405

pii

S0960894X01006679

journal_volume

12

pub_type

杂志文章

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