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ID: ALA1133050

Journal: Bioorg Med Chem Lett

Title: Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists.

Authors: Lagu B, Tian D, Chiu G, Nagarathnam D, Fang J, Shen Q, Forray C, Ransom RW, Chang RS, Vyas KP, Zhang K, Gluchowski C.

Abstract: Furo[3,4-d]pyrimidinones were found to be metabolites of dihydropyrimidinones such as 1a-b that are subtype-selective antagonists of the alpha1a-adrenergic receptor. A versatile synthesis that provides access to furo[3,4-d]pyrimidinones in high yield and in enantiomerically pure forms is described along with structure-activity relationships in the series.

CiteXplore: 10673105

DOI: 10.1016/s0960-894x(99)00653-8