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