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2-Aminothiazole based P2Y1 antagonists as novel antiplatelet agents |
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| Authors: | Zulan Pi James Sutton John Lloyd Ji Hua Laura Price Qimin Wu Ming Chang Joanna Zheng Robert Rehfuss Christine S Huang Ruth R Wexler Patrick YS Lam |
| Institution: | Medicinal Chemistry, Molecular Sciences and Candidate Optimization, Bristol-Myers Squibb, 311 Pennington-Rocky Hill Road, Pennington, NJ 08534, USA |
| Abstract: | ADP receptors, P2Y1 and P2Y12 have been recognized as potential targets for antithrombotic drugs. A series of P2Y1 antagonists that contain 2-aminothiazoles as urea surrogates were discovered. Extensive SAR of the thiazole ring is described. The most potent compound 7j showed good P2Y1 binding (Ki = 12 nM), moderate antagonism of platelet aggregation (PA IC50 = 5.2 μM) and acceptable PK in rats. |
| Keywords: | Platelet aggregation Antithrombotic Aminothiazole as urea surrogates |
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