Synthesis and antibacterial activity of novel ketolides with 11,12-quinoylalkyl side chains |
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| Authors: | Zhe-hui Zhao Xiao-xi Zhang Long-long Jin Shuang Yang Ping-sheng Lei |
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| Affiliation: | State Key Laboratory of Bioactive Substance and Function of Natural Medicines, Beijing Key Laboratory of Active Substances Discovery and Drugability Evaluation, Department of Medicinal Chemistry, Institute of Materia Medica, Peking Union Medical College & Chinese Academy of Medical Sciences, Beijing 100050, PR China |
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| 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. |
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| Keywords: | Ketolides Antibacterial activity Arylalkyl side chain |
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