Design, synthesis, and structure-activity relationships of phthalimide-phenylpiperazines: a novel series of potent and selective α1a-adrenergic receptor antagonists

…, WV Murray, V Pulito, L Jolliffe, P Cheung…

Index: Kuo, Gee-Hong; Prouty, Catherine; Murray, William V.; Pulito, Virginia; Jolliffe, Linda; Cheung, Peter; Varga, Sally; Evangelisto, Mary; Wang, Jian Journal of Medicinal Chemistry, 2000 , vol. 43, # 11 p. 2183 - 2195

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Citation Number: 25

Abstract

Beginning from the screening hit and literature α1-adrenergic compounds, a hybridized basic skeleton A was proposed as the pharmacophore for potent and selective α1a-AR antagonists. Introduction of a hydroxy group to increase the flexibility afforded B which served as the screening model and resulted in the identification of the second-generation lead 1. Using the Topliss approach, a number of potent and selective α1a-AR antagonists ...