Synthesis and antibacterial activity of novel ketolides with 11,12-quinoylalkyl side chains.
Synthesis and antibacterial activity of novel ketolides with 11,12-quinoylalkyl side chains.
Bioorg Med Chem Lett. 2018 Jun 19;:
Authors: Zhao ZH, Zhang XX, Jin LL, Yang S, Lei PS
Abstract
A series of quinoylalkyl side chains was designed and synthesized, followed by introduction into ketolides by coupling with building block 6 or 32. The corresponding targets 7a-n, 33b, and 33e 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 activity to telithromycin. Among them, two C2-F ketolides, compounds 33b and 33e, displayed excellent activities against macrolide-sensitive and macrolide-resistant pathogens.
PMID: 29937059 [PubMed - as supplied by publisher]
Source: Bioorganic and Medicinal Chemistry Letters - Category: Chemistry Authors: Zhao ZH, Zhang XX, Jin LL, Yang S, Lei PS Tags: Bioorg Med Chem Lett Source Type: research