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N,N'-双(2-羟基苄基)-1,2-乙二胺衍生物的合成与抗菌活性

Synthesis and Antimicrobial Activity of N,N'-Bis(2-hydroxylbenzyl)-1,2-ethanediamine Derivatives.

作者信息

Musa Musiliyu A, Khan M Omar F, Aspedon Arden, Cooperwood John S

机构信息

Florida A and M University, College of Arts and Sciences, Department of Chemistry, 219 Jones Halls, Tallahassee, FL 32307, USA; Tel: (1)-850-599-3509.

出版信息

Lett Drug Des Discov. 2010 Mar;7(3):165-170. doi: 10.2174/157018010790596678.

Abstract

A series of N,N'-Bis(2-hydroxylbenzyl)-1,2-ethanediamine derivatives and its schiff bases were synthesized, characterized and screened for in vitro antimicrobial activity against Staphylococcus aureus, Pseudomonas aeruginosa and Salmonella enterica. Result indicated that the ethylenediamine derivatives, N,N'-Bis(2-hydroxy-5-bromobenzyl)-1,2-ethanediamine (21), and N,N'-Bis(2-hydroxy-5-chlorobenzyl)-1,2-ethanediamine (22) showed the most favorable antimicrobial activity exhibiting LC(50) of 11.6 and 8.79 muM against S.enterica, 86 and 138 muM against P. aeruginosa, and 140 and 287 muM against S. aureus, respectively. These compounds displayed highest level of resistance with S. aureus. Thus, the high level of activity seen with the compounds (21, 22) suggests that these compounds could serve as the leads for development of novel synthetic compounds with enhanced antimicrobial activity.

摘要

合成了一系列N,N'-双(2-羟基苄基)-1,2-乙二胺衍生物及其席夫碱,对其进行了表征,并筛选了它们对金黄色葡萄球菌、铜绿假单胞菌和肠炎沙门氏菌的体外抗菌活性。结果表明,乙二胺衍生物N,N'-双(2-羟基-5-溴苄基)-1,2-乙二胺(21)和N,N'-双(2-羟基-5-氯苄基)-1,2-乙二胺(22)表现出最有利的抗菌活性,对肠炎沙门氏菌的半数致死浓度(LC(50))分别为11.6和8.79 μM,对铜绿假单胞菌为86和138 μM,对金黄色葡萄球菌为140和287 μM。这些化合物对金黄色葡萄球菌表现出最高水平的耐药性。因此,化合物(21,22)所呈现的高活性表明,这些化合物可作为开发具有增强抗菌活性的新型合成化合物的先导物。

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