2-Acylimino-3H-thiazoline derivatives: a novel template for platelet GPIIb/IIIa receptor antagonists |
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Authors: | Manaka A Sato M Aoki M Tanaka M Ikeda T Toda Y Yamane Y Nakaike S |
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Affiliation: | Taisho Pharmaceutical Co. Ltd., Medicinal Research Laboratories, Omiya-shi, Saitama, Japan. |
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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 beta-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 microM). |
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