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

Longlong Jin, Xiaoxi Zhang, Zhigang Luo, Xianfu Wu, Zhehui Zhao

Bioorganic & medicinal chemistry letters 2023 Jan 15

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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. Copyright © 2022 Elsevier Ltd. All rights reserved.

Citation

Longlong Jin, Xiaoxi Zhang, Zhigang Luo, Xianfu Wu, Zhehui Zhao. Synthesis and antibacterial activity of novel 2‑fluoro ketolide antibiotics with 11,12‑quinoylalkyl side chains. Bioorganic & medicinal chemistry letters. 2023 Jan 15;80:129115