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Updated: Oct 2, 2026

Split-and-pool Synthesis and Characterization of Peptide Tertiary Amide Library
Published on: June 20, 2014
Noncovalent tripeptidic thrombin inhibitors incorporating amidrazone, amine and amidine functions at P1
Koo Lee1, Won-Hyuk Jung, Cheol Won Park
1Life 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.
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