Bioorganic and Medicinal Chemistry Letters p. 1017 - 1022 (2002)
Update date:2022-08-04
Topics:
Lee, Koo
Jung, Won-Hyuk
Park, Cheol Won
Park, Hee Dong
Lee, Sun Hwa
Kwon, O Hwan
A series of noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1 was investigated. While the amidrazone and the amine series displayed limited oral absorption, the amidine series demonstrated generally good oral absorption and strong antithrombotic activity; the single-digit picomolar Ki achieved from this series is among the best yet reported. The present work highlights the benzamidine compound 11f (LB30812) that exhibits excellent overall profiles of potency, oral absorption and antithrombotic efficacy.
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