Design, synthesis, pharmacological evaluation, and docking study of new acridone-based 1,2,4-oxadiazoles as potential anticonvulsant agents
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- 作者：Maryam Mohammadi-Khanaposhtania ; Mohammad Shabanib ; Mehrdad Faizic ; Iraj Aghaeid ; Reza Jahanic ; Zainab Sharafie ; Narges Shamsaei Zafarghandia ; Mohammad Mahdavia ; Tahmineh Akbarzadeha ; f ; Saeed Emamig ; Abbas Shafieea ; Alireza Foroumadia ; h ; aforoumadi@yahoo.com" class="auth_mail" title="E-mail the corresponding author
- 关键词：Anticonvulsant agents ; Acridone ; Benzodiazepine (BZD) receptors ; Docking study ; 1 ; 2 ; 4-Oxadiazole
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：13 April 2016
- 年：2016
- 卷：112
- 期：Complete
- 页码：91-98
- 全文大小：578 K
文摘
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A series of acridone-based oxadiazoles were synthesized as anticonvulsant agents.
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All compounds were evaluated by MES, PTZ, neurotoxicity and cytotoxicity assays.
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4-MeO-phenyl analogs 11l and 11m were the most active compounds in PTZ test.
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Compounds 11b and 11m were the most active ones in MES test (ED50s ≤ 2.42 mg/kg).
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In vivo and in silico studies confirm binding of compound 11l with BZD receptors.