Synthesis and Biological Activity of Oximes, Amines, and Lactams of Fusidane Triterpenoids

Abstract

AbstractThe 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.