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Yulia V. Kozlova, Anastasia V. Knyazeva, Ulyana A. Budanova, Yurii L. Sebyakin
Cationic antimicrobial peptidomimetics based on L-lysine
and aliphatic derivatives of enantiomers of valine and leucine
Abstract
Abstract. It has been
established that a number of pathogenic bacterial strains, such as ESCAPE, can
easily acquire resistance to traditional antibiotics. This leads to the
emergence of multidrug resistance without currently available effective
treatment of the diseases they cause. Antimicrobial resistance is becoming a
global problem and requires the search for new approaches to solving this
problem. Research in recent decades has focused on the use of AMPs and
low-molecular peptidomimetics as compounds with promising potential activity
against pathogenic bacteria. The paper presents data on the prospects for
further development and use of lipodipeptides based on L-lysine derivatives and
optical isomers of esters of aliphatic amino acids valine and leucine. It is
shown that the synthesized cationic amphiphiles exhibit a high level of
activity against test gram-positive and gram-negative bacteria. No significant
differences in the efficiency of optical isomers of the two amino acid
derivatives were found. The determining factor in the activity of the samples
is obviously a slightly higher level of hydrophobicity of the cationic
lipodipeptides LysValCn and LysLeuCn with a difference in the length of the
hydrocarbon radicals of the obtained compounds.
Key words: cationic
amphiphiles, peptidomimetics, lipodipeptides, optical activity of amino acid
derivatives, antibacterial activity
Copyright (C) Chemistry Dept., Moscow State University, 2002
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