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KMID : 0043320130360060671
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Archives of Pharmacal Research
2013 Volume.36 No. 6 p.671 ~ p.683
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Novel 4-substituted-2(1H)-phthalazinone derivatives: synthesis, molecular modeling study and their effects on α-receptors
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Khalil Nadia A.
Ahmed Eman M.
Elshihawy Hosam A.
Zaitone Sawsan A.
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Abstract
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Novel 4-(4-bromophenyl)phthalazine derivatives connected via an alkyl spacer to amine or N-substituted piperazine were designed and synthesized as promising α-adrenoceptor antagonists. The structures of the phthalazine derivatives were established using elemental and spectral analyses. Twelve of the tested compounds displayed significant α-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.
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KEYWORD
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Phthalazinones, α-Adrenoceptor antagonists, Molecular modeling, Arylpiperazine
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