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Some novel josamycin derivatives bearing an arylalkyl-type side chain were designed and synthesized. By HWE or Wittig reaction, 16-aldehyde group of josamycin analogs were converted into unsaturated carbonyl compounds. They were evaluated for their in vitro antibacterial activities against a panel of respiratory pathogens. 8b and 8e exhibited comparable activities against a panel of respiratory pathogens, especially to resistant ones in the series of desmycarosyl josamycin analogs. Among of all the target molecules, 21 showed the best antibacterial activities.

Citation

Zhe-Hui Zhao, Long-Long Jin, Yan-Peng Xu, Chao Liu, A-Peng Wang, Ping-Sheng Lei. Synthesis and antibacterial activities of some novel 17, 18-unsaturated carbonyl compounds derivated from josamycin. Journal of Asian natural products research. 2017 Apr;19(4):358-387

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PMID: 28276768

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