Selective α 1a adrenergic receptor antagonists based on 4-aryl-3, 4-dihydropyridine-2-ones

…, RSL Chang, SS O'Malley, DR Reiss, TP Broten…

文献索引：Nantermet; Barrow; Selnick; Homnick; Freidinger; Chang; O'Malley; Reiss; Broten; Ransom; Pettibone; Olah; Forray Bioorganic and medicinal chemistry letters, 2000 , vol. 10, # 15 p. 1625 - 1628

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被引用次数: 26

摘要

A series of α1a receptor antagonists derived from a 4-aryl-3, 4-dihydropyridine-2-one heterocycle is disclosed. Potency in the low nanomolar to picomolar range along with high selectivity was obtained. In vivo efficacy in a prostate contraction model in rats was observed with a few derivatives.