Novel 4-substituted-2(1H)-phthalazinone derivatives: synthesis, molecular modeling study and their effects on alpha-receptors

作者：Khalil Nadia A; Ahmed Eman M^*; Elshihawy Hosam A; Zaitone Sawsan A

来源：Archives of Pharmacal Research, 2013, 36(6): 671-683.

DOI：10.1007/s12272-013-0095-5

• Phthalazinones
• alpha-Adrenoceptor antagonists
• Molecular modeling
• Arylpiperazine

Novel 4-(4-bromophenyl)phthalazine derivatives connected via an alkyl spacer to amine or N-substituted piperazine were designed and synthesized as promising alpha-adrenoceptor antagonists. The structures of the phthalazine derivatives were established using elemental and spectral analyses. Twelve of the tested compounds displayed significant alpha-blocking activity. Molecular modeling studies were performed to rationalize the biological results. Among the tested compounds, 7j displayed the best-fitting score and the highest in vitro activity.

• 出版日期2013-6