Department of Chemistry, University of Delhi, Delhi 110007, India.
Eur J Med Chem. 2011 Feb;46(2):480-7. doi: 10.1016/j.ejmech.2010.11.027. Epub 2010 Nov 24.
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.
我们在此报告一系列 N,N-二苄基环己烷-1,2-二胺衍生物的合成和抗菌活性。为了研究取代的二苄基环己烷-1,2-二胺衍生物的构效关系，合成了 44 种结构多样的化合物，并对革兰氏阳性和革兰氏阴性细菌菌株进行了测试。其中，化合物 17-20、26、37、38 的活性比四环素更强，MIC 值范围为 0.0005-0.032μg/mL，在哺乳动物红细胞中未观察到溶血，最高可达 1024μg/mL。一些化合物还对白色念珠菌、光滑念珠菌和近平滑念珠菌表现出非常有前景的抗真菌活性。
