2-Acylimino-3H-thiazoline derivatives : A novel template for platelet GPIIb/IIIa receptor antagonists

Abstract In the course of our research for the low-molecular weight RGD peptide mimics, we have found that a rigid 2-acylimino-3 H -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)-3 H -thiazoline-5-carboxamide ( 7c ), namely PS-028 ( K i =46.5±5.8 pM).