Phenylacetamides as selective α-1A adrenergic receptor antagonists

…, D Nagarathnam, C Forray, C Gluchowski…

文献索引：Patane, Michael A.; DiPardo, Robert M.; Newton, Randall C.; Price, RoseAnn P.; Broten, Theodore P.; Chang, Raymond S.L.; Ransom, Richard W.; Di Salvo, Jerry; Nagarathnam, Dhanapalan; Forray, Carlos; Gluchowski, Charles; Bock, Mark G. Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 15 p. 1621 - 1624

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被引用次数: 11

摘要

A novel class of potent and selective α-1a receptor antagonists has been identified. The structures of these antagonists were derived from truncating the 4-aryl dihydropyridine subunit present in known α-1a antagonists. The design principles which led to the discovery of substituted phenylacetamides, the synthesis and SAR of key analogues, and the results of select in vitro and in vivo studies are described.