Antibacterial activities of a series of novel 5-O-(4′, 6′-O-dimodified)-mycaminose 14-membered ketolides

Zhe-Hui ZhaoState 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, Beijing100050, ChinaCorrespondence[email protected]

A-Peng WangState 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, Beijing100050, China

Xiao-Xi ZhangState 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, Beijing100050, China

Shuang YangState 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, Beijing100050, China

Zhi-Gang LuoState 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, Beijing100050, China

Ping-Sheng LeiState 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, Beijing100050, China

Abstract

A series of novel 5-O-(4′,6′-O-dimodified)-mycaminose 14-membered ketolides were assessed for their in vitro antibacterial activities against a panel of sensitive and resistant pathogens. Compound 1 and compound 2, two ester analogs, showed the best antibacterial activities against several macrolide-sensitive and macrolide-resistant strains. These results indicated that introducing ester to 6-OH and a small volume ether substituent to the 4-OH of mycaminose could improve the antibacterial activities of ketolides.

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Acknowledgments

We are grateful to the Department of Instrumental Analysis of our institute for performing the NMR and mass spectroscopy measurements.

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Antibacterial activities of a series of novel 5-O-(4′, 6′-O-dimodified)-mycaminose 14-membered ketolides

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Antibacterial activities of a series of novel 5-O-(4′, 6′-O-dimodified)-mycaminose 14-membered ketolides

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