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ID: ALA3351863

Journal: Bioorg Med Chem Lett

Title: Optimization of 2-phenyl-pyrimidine-4-carboxamides towards potent, orally bioavailable and selective P2Y(12) antagonists for inhibition of platelet aggregation.

Authors: Caroff E, Meyer E, Treiber A, Hilpert K, Riederer MA.

Abstract: 2-Phenyl-pyrimidine-4-carboxamide analogs were identified as P2Y12 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.

CiteXplore: 25113932

DOI: 10.1016/j.bmcl.2014.06.070