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Discovery of new hazimycin congeners from Kitasatospora sp.P07101

Acta Pharmaceutica Sinica B 2015年第6期5卷 564-568页

作者： nobuhiro koyama Hirofumi Sato Hiroshi Tomoda Graduate School of Pharmaceutical Sciences Kitasato University

In an analytical study of microbial broths,the actinomycete strain Kitasatospora sp.P07101 was found to produce three new congeners,which were designated hazimycins B(1),C(2),and D(3),together with the previously reported hazimycin(renamed hazimycin A(4)).The structures of these hazimycins were examined using various spectroscopic methods including nuclear magnetic resonance(NMR),and the results revealed that 1–3 were analogues of hazimycin with the replacement of one of the two isonitrile groups in 4 by an NH-formyl group in 1,the two isonitrile groups and an amide group by two NH-formyl groups and a nitrile group in 2,and the two isonitrile groups and two amide groups by two NH-formyl groups and two nitrile groups in *** hazimycin A exhibited moderate antimicrobial activities against Gram-positive bacteria and Candida *** results indicated that the presence of two isonitrile groups in the hazimycin structure is essential for antimicrobial activity.

关键词： Hazimycin Isonitrile Nitrile Microbial metabolites Kitasatospora

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New cyslabdans B and C, potentiators of imipenem activity against methicillin-resistant Staphylococcus aureus produced by Streptomyces sp. K04-0144

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Acta Pharmaceutica Sinica B 2011年第4期1卷 236-239页

作者： nobuhiro koyama Yuriko Tokura Yoko Takahashi Hiroshi Tomoda Graduate School of Pharmaceutical Sciences Kitasato UniversityTokyo 108-8641Japan Kitasato Institute for Life Sciences Kitasato UniversityTokyo 108-8641Japan

From a further purification study,two new congeners designated cyslabdans B(1)and C(2)were isolated along with previously reported cyslabdan(cyslabdan A(3)in this study)from the culture broth of Streptomyces *** structure was elucidated by various spectroscopy including NMR,revealing that 1 and 2 was 18-hydroxy and 10-methoxy cyslabdan,*** 1 and 2 were found to potentiate imipenem activity against methicillinresistant Staphylococcus aureus by 123 fold and 533 fold,*** with the activity of compound 3 indicated that the introduction of a hydrophilic group at the dimethyl moiety of the decalin ring was unfavorable for its activity.

关键词： Cyslabdan Actinomycete metabolites Imipenem potentiator Methicillin-resistant Staphylococcus aureus(MRSA)

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