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Synthesis and Biological Activity of Oximes, Amines, and Lactams of Fusidane Triterpenoids
Author(s) -
Salimova Elena V.,
Parfenova Lyudmila V.
Publication year - 2021
Publication title -
chemistryselect
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.437
H-Index - 34
ISSN - 2365-6549
DOI - 10.1002/slct.202102019
Subject(s) - oxime , chemistry , fusidic acid , beckmann rearrangement , antibiotics , antimicrobial , molecule , stereochemistry , caprolactam , bacteria , biochemistry , organic chemistry , biology , staphylococcus aureus , genetics
The article presents the synthesis and study of the antimicrobial and antitumor activity of fusidic acid derivatives containing oxime, amino substituents, and a caprolactam ring. The introduction of a caprolactam fragment into the molecule provides a high antibacterial effect comparable to that of fusidic acid and contributes to a 5.8‐fold decrease in hemolytic activity compared to that of the native antibiotic. The presence of two oxime groups in the methylfusidate molecule ensures a high antiproliferative effect against H522 cells of non‐small cell lung cancer, leading to 57 % of the lethality of this cell line.