N-Arylpiperazinyl-N'-propylamino Derivatives of Heteroaryl Amides as Functional Uroselective α1-Adrenoceptor Antagonists

…, L Sandoval, EB Sjogren, FX Talamás…

Index: Elworthy, Todd R.; Ford, Anthony P. D. W.; Bantle, Gary W.; Morgans Jr., David J.; Ozer, Rachel S.; Palmer, Wylie S.; Repke, David B.; Romero, Magarita; Sandoval, Leticia; Sjogren, Eric B.; Talamas, Francisco X.; Vazquez, Alfredo; Wu, Helen; Arredondo, Nicolas F.; Blue Jr., David R.; DeSousa, Andrea; Gross, Lisa M.; Kava, M. Shannon; Lesnick, John D.; Vimont, Rachel L.; Williams, Timothy J.; Zhu, Quan-Ming; Pfister, Juerg R.; Clarke, David E. Journal of Medicinal Chemistry, 1997 , vol. 40, # 17 p. 2674 - 2687

Full Text: HTML

Citation Number: 52

Abstract

Novel arylpiperazines were identified as α1-adrenoceptor (AR) subtype-selective antagonists by functional in vitro screening. 3-[4-(ortho-Substituted phenyl) piperazin-1-yl] propylamines were derivatized with N, N-dimethyl anthranilamides, nicotinamides, as well as carboxamides of quinoline, 1, 8-naphthyridine, pyrazolo [3, 4-b] pyridine, isoxazolo [3, 4- b] pyridine, imidazo [4, 5-b] pyridine, and pyrazolo [1, 5-a] pyrimidines. Strips of rabbit ...