期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 11, 页码 3338-3343出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.04.028
关键词
P2Y1 receptor; GPCR antagonist; antiplatelet; antithrombotic; cardiovascular disease
The P2Y(1) and P2Y(12) purinergic receptors are responsible for mediating adenosine diphosphate (ADP) dependent platelet aggregation. Evidence from P2Y(1) knockout studies as well as from nucleotide-based small molecule P2Y(1) antagonists has suggested that the antagonism of this receptor may offer a novel and effective method for the treatment of thrombotic disorders. Herein, we report the identification and optimization of a series of non-nucleotide P2Y(1) antagonists that are potent and orally bioavailable. (C) 2008 Elsevier Ltd. All rights reserved.
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