845524-65-4Relevant academic research and scientific papers
2-Acylimino-3-alkyl-3H-thiazoline derivatives: One-pot, three-component condensation synthesis of novel β-turn mimics
Manaka, Akira,Ishii, Takaaki,Takahashi, Keiko,Sato, Masakazu
, p. 419 - 422 (2007/10/03)
One-pot, three-component condensation of aroylthiourea, primary amine and α-halocarbonyl derivatives for the synthesis of 2-acylimino-3-alkyl-3H- thiazoline derivatives is described. This method is useful for simultaneously incorporating diverse functional groups at four positions in the 3H-thiazoline skeleton to obtain β-turn tripeptide mimics.
2-acylimino-3H-thiazoline derivatives: A novel template for platelet GPIIb/IIIa receptor antagonists
Manaka, Akira,Sato, Masakazu,Aoki, Mari,Tanaka, Makoto,Ikeda, Tomotake,Toda, Yoshihisa,Yamane, Yuuko,Nakaike, Shiro
, p. 1031 - 1035 (2007/10/03)
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-(4amidinobenzoylimino)-3,4-dimethyl-N-(2-carboxyethyl) -3H-thiazoline-5-carboxamide (7c), namely PS-028 (Ki = 46.5± 5.8 pM).
