Synthesis and evaluation of furo[3,4-d]pyrimidinones as selective alpha1a-adrenergic receptor antagonists |
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Authors: | Lagu B Tian D Chiu G Nagarathnam D Fang J Shen Q Forray C Ransom R W Chang R S Vyas K P Zhang K Gluchowski C |
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Institution: | Department of Chemistry, Synaptic Pharmaceutical Corporation, Paramus, NJ 07652, USA. |
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Abstract: | Furo3,4-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 furo3,4-d]pyrimidinones in high yield and in enantiomerically pure forms is described along with structure-activity relationships in the series. |
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