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

作者信息

Li Min-Yong, Fang Hao, Xia Lin

机构信息

Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.

出版信息

Bioorg Med Chem Lett. 2005 Jul 1;15(13):3216-9. doi: 10.1016/j.bmcl.2005.05.003.

DOI:10.1016/j.bmcl.2005.05.003
PMID:15935663
Abstract

Phenyl-piperazines were designed and synthesized based on pharmacophore for uro-selective alpha(1)-adrenoceptor antagonists and 3D chemical database searching. Within this series, three compounds, 2, 3, and 13, showed similar or better alpha(1)-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 alpha(1)-adrenoceptor antagonists, which can be used for the treatment of BPH with fewer side effects.

摘要

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