Design, Synthesis, and Activity Evaluation of C-23-Modified 5-<i>O</i>-Mycaminosyltylonolide Derivatives.

ABSTRACT: The widespread use of tylosin family drugs in clinical practice has led to bacterial resistance and reduced therapeutic efficacy. We designed and synthesized a series of new semisynthetic derivatives of tylosin with 5-O-mycaminosyltylonolide as the mother nucleus, mainly by introducing a variety of amino groups at its C-23 position. Some of the compounds showed high antibacterial activity against Gram-negative and Gram-positive bacteria. These findings indicate that the best compound, c9, possessed significant antibacterial activity (MIC = 0.5 ug/mL), excellent bactericidal efficacy, and a low induction rate of drug resistance against Staphylococcus aureus and Escherichia coli; it also showed good antibacterial activity against drug-resistant bacteria. In additi

SUBMITTER: Fan Z 

PROVIDER: S-EPMC11647724 | biostudies-literature | 2024 Dec

REPOSITORIES: biostudies-literature