Design, synthesis, molecular modeling and biological evaluation of novel 2,3-dihydrophthalazine-1,4-dione derivatives as potential anticonvulsant agents

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• 作者：Abdel Ghany A. El-Helby^a ; Rezk R. Ayyad^a ; ^b ; Helmy M. Sakr^a ; Adel S. Abdelrahim^a ; K. El-Adl^a ; Farag S. Sherbiny^c ; ^d ; Ibrahim H. Eissa^a ; ^{ibrahimeissa@azhar.edu.eg} ; Mohamed M. Khalifa^a ; ^{khalifa_mohamed22@yahoo.com}
• 关键词：2 ; 3-Dihydrophthalazine-1 ; 4-dione ; Molecular modeling ; Anticonvulsant ; GABA-A
• 刊名：Journal of Molecular Structure
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：1130
• 期：Complete
• 页码：333-351
• 全文大小：2914 K
• 卷排序：1130

文摘

Novel series of 2,3-Dihydrophthalazine-1,4-dione was designed and synthesized. Anticonvulsant activity was evaluated for all derivatives as GABA-A modulators. Compounds 13 and 14g are the most potent derivatives. Molecular modeling studies were performed to justify the biological activity.