Synthesis and biological evaluation of N-antipyrine-4-substituted amino-3-chloromaleimide derivatives

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• 作者：Fern ; a Mahle ; Tatiana da Rosa Guimar&#xe3 ; es ; Ale ; ra Vergilina Meira ; Rog&#xe9 ; rio Corr&#xea ; a ; Rosana C&#xe9 ; Bella Cruz ; Alex ; re Bella Cruz ; Ricardo Jos&#xe9 ; Nunes ; Valdir Cechinel-Filho ; F&#xe1 ; tima de Campos-Buzzi
• 关键词：Cyclic imides ; Antipyrine ; Antinociceptive activity ; Antimicrobial activity
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：November 2010
• 年：2010
• 卷：45
• 期：11
• 页码：4761-4768
• 全文大小：512 K

文摘

This paper describes the synthesis of new cyclic imides obtained by reaction with N-antipyrine-3,4-dichloromaleimides and different aromatic amines. The analgesic activity of the synthesized compounds was initially investigated against the writhing test in mice, followed by analysis of the most promising compounds in this model and in the formalin-induced model. The results indicate that the compounds containing the electron-withdrawing substituents in the para position of the substitute ring exerted more potent analgesic activity in mice, being much more potent than the prototype N-antipyrine-3,4-dichloromaleimide and some reference drugs. Some compounds exhibited activity against human opportunistic and pathogenic fungi, with MIC values of between 40 and 100 μg/mL (91.74 and 236.96 μM), and it was verified that only a few compounds presented potential for cytotoxic activity.