Design and synthesis of novel α1a adrenoceptor-selective dihydropyridine antagonists for the treatment of benign prostatic hyperplasia

…, X Hong, J Fang, C Forray, TA Branchek…

Index: Nagarathnam, Dhanapalan; Wetzel, John M.; Miao, Shou Wu; Marzabadi, Mohammad R.; Chiu, George; Wong, Wai C.; Hong, Xingfang; Fang, James; Forray, Carlos; Branchek, Theresa A.; Heydorn, William E.; Chang, Raymond S. L.; Broten, Theodore; Schorn, Terry W.; Gluchowski, Charles Journal of Medicinal Chemistry, 1998 , vol. 41, # 26 p. 5320 - 5333

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Citation Number: 57

Abstract

We report the synthesis and evaluation of novel α1a adrenoceptor subtype-selective antagonists. Systematic modification of the lipophilic 4, 4-diphenylpiperidinyl moiety of the dihydropyridine derivatives 1 and 2 provided several highly selective and potent α1a antagonists. From this series, we identified the 4-(methoxycarbonyl)-4-phenylpiperidine analogue SNAP 5540 (-)[(-)-63] for further characterization. When examined in an isolated ...