Antibacterial Activity of Amphiphiles Based on Indolyl-3-Carboxylic Acids and L-Lysine with an Ethylenediamine Linker

IF 0.7 Q4 CHEMISTRY, MULTIDISCIPLINARY
V. O. Ovsyannikov, A. Yu. Mikhailova, U. A. Budanova, Yu. L. Sebyakin
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引用次数: 0

Abstract

Recently, due to the growth in bacterial infections resistant to antibiotics, there is an urgent need for developing alternative antibacterial drugs. Alkyl-indolyl-L-lysines are a promising class of compounds; their amphiphilic structure is crucial in antimicrobial efficacy. A scheme is developed and five new derivatives of indolylbutyric and indolylacetic acids containing a polar amino acid residue with an ethylenediamine linker binding alkyl fragments with different lengths are synthesized. The antibacterial activity of the new amphiphiles against gram-positive and gram-negative bacterial strains is evaluated. The minimum binding energy of the synthesized compounds with human serum albumin (HSA) is determined by molecular docking. A lower affinity of the studied objects in comparison with control indolmycin is shown.

Abstract Image

Abstract Image

基于吲哚基-3-羧酸和 L-赖氨酸与乙二胺连接体的双亲化合物的抗菌活性
摘要近年来,由于细菌感染对抗生素的耐药性不断增加,因此迫切需要开发替代抗菌药物。烷基吲哚-L-赖氨酸是一类很有前途的化合物;其两亲性结构对抗菌效果至关重要。本研究开发了一种方案,并合成了五种新的吲哚丁酸和吲哚乙酸衍生物,这些衍生物含有一个极性氨基酸残基和一个结合不同长度烷基片段的乙二胺连接体。评估了新型双亲化合物对革兰氏阳性和革兰氏阴性细菌菌株的抗菌活性。通过分子对接确定了合成化合物与人血清白蛋白(HSA)的最小结合能。结果表明,与对照吲哚霉素相比,所研究对象的亲和力较低。
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来源期刊
Moscow University Chemistry Bulletin
Moscow University Chemistry Bulletin CHEMISTRY, MULTIDISCIPLINARY-
CiteScore
1.30
自引率
14.30%
发文量
38
期刊介绍: Moscow University Chemistry Bulletin is a journal that publishes review articles, original research articles, and short communications on various areas of basic and applied research in chemistry, including medical chemistry and pharmacology.
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