Synthesis, antimicrobial activity and structure–activity relationship study of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives

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• 作者：Mukul Sharma ; Penny Joshi ; Nitin Kumar ; Seema Joshi ; Rajesh K. Rohilla ; Nilanjan Roy ; Diwan S. Rawat
• 关键词：Antibacterial ; Antifungal ; Hemolysis
• 刊名：European Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：February 2011
• 年：2011
• 卷：46
• 期：2
• 页码：480-487
• 全文大小：313 K

文摘

We report herein synthesis and antimicrobial activity of a series of N,N-dibenzyl-cyclohexane-1,2-diamine derivatives. In order to study the structure–activity relationship of substituted dibenzyl-cyclohexane-1,2-diamine derivatives, 44 structurally diverse compounds were synthesized and tested against Gram-positive and Gram-negative bacterial strains. Among them, compounds 17-20, 26, 37, 38 were found to be more active than tetracycline with MIC value ranging 0.0005–0.032 μg/mL and no hemolysis upto 1024 μg/mL in mammalian erythrocytes was observed. Some of the compounds have also shown very promising antifungal activity against Candida albicans, Candida glabrata and Geotrichum candidium.