Bioorganic & medicinal chemistry letters

Pharmacophore-based design, synthesis, biological evaluation, and 3D-QSAR studies of aryl-piperazines as α 1-adrenoceptor antagonists

MY Li, H Fang, L Xia

Index: Li, Min-Yong; Fang, Hao; Xia, Lin Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 13 p. 3216 - 3219

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Citation Number: 37

Abstract

Phenyl-piperazines were designed and synthesized based on pharmacophore for uro- selective α1-adrenoceptor antagonists and 3D chemical database searching. Within this series, three compounds, 2, 3, and 13, showed similar or better α1-AR antagonistic activity compared with prazosin. The 3D-QSAR study of these compounds may provide useful information for the development of novel aryl-piperazines as uro-selective α1- ...