Synthesis and antibacterial activity of novel 2‑fluoro ketolide antibiotics with 11,12‑quinoylalkyl side chains

Bioorg Med Chem Lett. 2023 Jan 15:80:129115. doi: 10.1016/j.bmcl.2022.129115. Epub 2022 Dec 24.

Abstract

A series of novel 2‑fluoro ketolide antibiotics with 11,12‑quinoylalkyl side chains derived from telithromycin and cethromycin were designed and synthesized. The corresponding targets 2a-o were tested for their in vitro activities against a series of macrolide-sensitive and macrolide-resistant pathogens. Some of them showed a similar antibacterial spectrum and comparable or slightly better activity to telithromycin. Among them, compounds 2g and 2k, displayed excellent activities against macrolide-sensitive and macrolide-resistant pathogens.

Keywords: Antibacterial activity; Cethromycin; Ketolides; Synthesis; Telithromycin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Anti-Bacterial Agents / chemistry
  • Ketolides*
  • Macrolides
  • Microbial Sensitivity Tests
  • Quinolines

Substances

  • Anti-Bacterial Agents
  • Ketolides
  • Macrolides
  • telithromycin
  • Quinolines