Cationic Lipoaminoacid Derivatives of Diethanolamine as Potentially Membrane-Active Antibacterial Agents

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This work is aimed to develop a number of cationic amphiphiles based on amino acid derivatives of diethanolamine as potentially membrane-active antibacterial agents. The developed compounds contain two amino acid residues in the polar block and various length of aliphatic chains in the hydrophobic domain. Amphiphiles were obtained in preparative amounts sufficient to confirm their structures and perform a study of antibacterial activity. The synthesized samples based on β-Ala (4c) and GABA (4d) with an aliphatic C12 chain in the hydrophobic domain showed a promising level of antimicrobial activity (minimal inhibitory concentration, MIC, 1 μg/mL) against gram-positive (B. subtilis) and gram-negative (E. coli) bacteria. Amphiphiles containing aromatic amino acids L-Phe (6a) and L-Trp (6b) in the polar head group and C8 hydrocarbon chain are active against B. subtilis with a MIC of 1 μg/mL. The obtained data on antimicrobial activity make the selected compounds attractive for further detailed study of their mechanism of action.

作者简介

M. Guseva

MIREA, Russian Technology University, Lomonosov Institute of Fine Chemical Technology

Email: c-221@yandex.ru
Russia, 119571, Moscow

Z. Denieva

Frumkin Institute of Physical Chemistry and Electrochemistry, Russian Academy of Sciences

Email: c-221@yandex.ru
Russia, 119071, Moscow

U. Budanova

MIREA, Russian Technology University, Lomonosov Institute of Fine Chemical Technology

编辑信件的主要联系方式.
Email: c-221@yandex.ru
Russia, 119571, Moscow

Yu. Sebyakin

MIREA, Russian Technology University, Lomonosov Institute of Fine Chemical Technology

Email: c-221@yandex.ru
Russia, 119571, Moscow

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