Synthesis and biological evaluation of a new series of N -acyldiamines as potential antibacterial and antifungal agents
作者:Bianca da S. Ferreira、Angelina M. de Almeida、Thiago C. Nascimento、Pedro P. de Castro、Vania L. Silva、Claúdio G. Diniz、Mireille Le Hyaric
DOI:10.1016/j.bmcl.2014.08.047
日期:2014.10
In continuation of our efforts to find new antimicrobial compounds, series of fatty N-acyldiamines were prepared from fatty methyl esters and 1,2-ethylenediamine, 1,3-propanediamine or 1,4-butanediamine. The synthesized compounds were screened for their antibacterial activity against Gram-positive bacteria (Staphylococcus aureus, Staphylococcus epidermidis), Gram-negative bacteria (Escherichia coli
为了继续努力寻找新的抗菌化合物,从脂肪甲酯和1,2-乙二胺,1,3-丙二胺或1,4-丁二胺制备了一系列的脂肪N-酰基二胺。筛选合成的化合物对革兰氏阳性菌(金黄色葡萄球菌,表皮葡萄球菌),革兰氏阴性菌(大肠杆菌,铜绿假单胞菌)的抗菌活性以及对四种念珠菌(C. albicans,C.热带,光滑念珠菌和近平滑念珠菌)。化合物5a(N-(2-氨基乙基)十二碳酰胺),5b(N-(2-氨基乙基)四碳酰胺)和6d(N-(3-氨基丙基)油酰胺)对革兰氏阳性细菌的活性最高,MIC值为1至16并评估其对21种耐甲氧西林金黄色葡萄球菌临床分离株的活性。所有化合物均表现出良好至中等的抗真菌活性。与氯霉素相比,化合物6b表现出相似的活性(MIC 50 = 16μg/ mL)。亲脂性和生物学活性之间可以建立正相关。