Synthesis and Evaluation of the Antimicrobial Activity of Cationic Amphiphiles Based on Bivalent Diethylenetriamine Derivatives

被引:0
|
作者
Guseva, M. K. [1 ]
Budanova, U. A. [1 ]
Sebyakin, Yu. L. [1 ]
机构
[1] Russian Technol Univ, Lomonosov Inst Fine Chem Technol, MIREA, 66 Vernadskogo Prosp, Moscow 119571, Russia
基金
俄罗斯基础研究基金会;
关键词
cationic amphiphiles; diethylenetriamine derivatives; antibacterial activity; ANTIBACTERIAL; MIMICS; DESIGN;
D O I
10.1007/s11094-023-02834-z
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The values of the hydrophilic(lipophilic balance (HLB) of various amino-acid derivatives of diethylenetriamine were calculated. Compounds with HLB indices within the range of manifestation of potential antimicrobial activity were selected from the library. Cationic amphiphiles containing fragments of aromatic (L-Phe, L-Trp) and aliphatic amino acids (gamma-aminobutyric acid, GABA) were synthesized. The antibacterial activity was preliminarily studied on Gram-positive B. subtilis 534 and Gram-negative E. coli M17 bacteria by the serial microdilution method. The most active compound had an aliphatic GABA amino-acid residue and an elongated diethylenetriamine derivative with a C12 alkyl chain.
引用
收藏
页码:1607 / 1612
页数:6
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