Pharmacophore-based design, synthesis, biological evaluation, and 3D-QSAR studies of aryl-piperazines as alpha(1)-adrenoceptor antagonists.
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.
Li
Min-Yong
MY
Department of Medicinal Chemistry, China Pharmaceutical University, Nanjing 210009, China.
Fang
Hao
H
Xia
Lin
L
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists / Q000138:chemical synthesis* / Q000494:pharmacology; D016208:Databases, Factual; D015195:Drug Design; D006801:Humans; D008297:Male; D010879:Piperazines / Q000138:chemical synthesis* / Q000494:pharmacology; D011224:Prazosin; D011470:Prostatic Hyperplasia / Q000188:drug therapy; D021281:Quantitative Structure-Activity Relationship; D013329:Structure-Activity Relationship
D058668:Adrenergic alpha-1 Receptor Antagonists; D000317:Adrenergic alpha-Antagonists; D010879:Piperazines; D011224:Prazosin