Author/Authors :
Akira Manaka، نويسنده , , Masakazu Sato، نويسنده , , Mari Aoki، نويسنده , , Makoto Tanaka، نويسنده , , Tomotake Ikeda، نويسنده , , Yoshihisa Toda، نويسنده , , Yuuko Yamane، نويسنده , , Shiro Nakaike، نويسنده ,
Abstract :
In the course of our research for the low-molecular weight RGD peptide mimics, we have found that a rigid 2-acylimino-3H-thiazoline structure is suitable for the peptide backbone mimics. Introduction of amidinophenyl and β-alanine moiety as arginine and aspartic acid side-chain surrogates to this backbone mimic resulted in a highly potent fibrinogen receptor antagonist 2-(4-amidinobenzoylimino)-3,4-dimethyl-N-(2-carboxyethyl)-3H-thiazoline-5-carboxamide (7c), namely PS-028 (Ki=46.5±5.8 pM).
