Cationic Antimicrobial Peptidomimetics Based in L-Lysine and Aliphatic Derivatives of Enantiomers of Valine and Leucine

Abstract

It is established that several 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 a search for new approaches to solve this problem. Research in recent decades has focused on the use of antimicrobial peptides (AMPs) and low-molecular peptidomimetics as compounds with promising potential activity against pathogenic bacteria. This study 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 are found. The determining factor in the activity of the samples is the 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.