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

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 o...

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Bibliographic Details
Published inPharmaceutical chemistry journal Vol. 56; no. 12; pp. 1607 - 1612
Main Authors Guseva, M. K., Budanova, U. A., Sebyakin, Yu. L.
Format Journal Article
LanguageEnglish
Published New York Springer US 01.03.2023
Springer
Subjects
Antibacterial agents
Fine chemicals
GABA
Medicine
Organic Chemistry
Pharmacology/Toxicology
Pharmacy
antibacterial activity
diethylenetriamine derivatives
cationic amphiphiles
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Summary: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 (γ-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.
ISSN:0091-150X
1573-9031
DOI:10.1007/s11094-023-02834-z