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Updated: Aug 17, 2026

Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Pharmacophore-based design, synthesis, biological evaluation, and 3D-QSAR studies of aryl-piperazines as
Min-Yong Li1, Hao Fang, Lin Xia
1Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
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.
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