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

Bioorg Med Chem Lett. 2022 Dec 24:129115. doi: 10.1016/j.bmcl.2022.129115. Online ahead of print.ABSTRACTA 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.PMID:36574853 | DOI:10.1016/j.bmcl.2022.129115
Source: Bioorganic and Medicinal Chemistry Letters - Category: Chemistry Authors: Source Type: research