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Vyacheslav O. Ovsyannikov, Anastasia Yu. Mikhailova, Ulyana A. Budanova, Yurii L. Sebyakin
Antibacterial
activity of amphiphiles based on indolyl-3-carboxylic acids and l-lysine with
ethylenediamine linker
Abstract
Abstract. Recently, due to the growth of bacterial infections resistant to
antibiotics, there is an urgent need to develop alternative antibacterial
drugs. Alkyl-indolyl-L-lysine is a promising class of compounds; their
amphiphilic structure is key in antimicrobial efficacy. A scheme was developed
and the synthesis of five new derivatives of indolylbutyric and indolylacetic
acids containing a polar amino acid residue with an ethylenediamine linker
binding alkyl fragments of different lengths was carried out. The antibacterial
activity of new amphiphiles against gram-positive and gram-negative bacterial
strains was evaluated. The minimum binding energy of synthesized compounds with
human serum albumin (HSA) was determined by the method of molecular docking. A
lower affinity of the studied objects was shown compared to the control
indolmycin.
Key words: indol-3-carboxylic acids, alkyl-indolyl-L-lysine,
amphiphiles, antibacterial activity
Copyright (C) Chemistry Dept., Moscow State University, 2002
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