Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1 |
| |
Authors: | Lee Koo Jung Won-Hyuk Park Cheol Won Park Hee Dong Lee Sun Hwa Kwon O Hwan |
| |
Affiliation: | Life Science R&D, LGCI, PO Box 61 Yu-Sung, Science Town, Taejon 305-380, Republic of Korea.kleec@lgci.co.kr |
| |
Abstract: | 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 K(i) 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. |
| |
Keywords: | |
本文献已被 ScienceDirect PubMed 等数据库收录! |
|