期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 23, 期 14, 页码 4206-4209出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2013.05.025
关键词
P2Y(1) antagonists; Platelet aggregation; Antithrombotic; Aminothiazole as urea surrogates
ADP receptors, P2Y(1) and P2Y(12) have been recognized as potential targets for antithrombotic drugs. A series of P2Y(1) 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 P2Y(1) binding (K-i = 12 nM), moderate antagonism of platelet aggregation (PA IC50 = 5.2 mu M) and acceptable PK in rats. (C) 2013 Elsevier Ltd. All rights reserved.
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