期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 24, 期 17, 页码 4323-4331出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.06.070
关键词
P2Y(12) receptor; P2Y(12) antagonist; GPCR antagonist; Antiplatelet; Antithrombotic
2-Phenyl-pyrimidine-4-carboxamide analogs were identified as P2Y(12) antagonists. Optimization of the carbon-linked or nitrogen-linked substituent at the 6-position of the pyrimidine ring provided compounds with excellent ex vivo potency in the platelet aggregation assay in human plasma. Compound 23u met the objectives for activity, selectivity and ADMET properties. (C) 2014 Elsevier Ltd. All rights reserved.
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