Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1

K Lee, WH Jung, CW Park, HD Park, SH Lee…

文献索引：Lee, Koo; Jung, Won-Hyuk; Park, Cheol Won; Park, Hee Dong; Lee, Sun Hwa; Kwon, O Hwan Bioorganic and Medicinal Chemistry Letters, 2002 , vol. 12, # 7 p. 1017 - 1022

全文：HTML全文

被引用次数: 17

摘要

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 ...