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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Novel streptopyrroles from Streptomyces rimosus with bacterial protein histidine kinase inhibitory and antimicrobial activities
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Novel streptopyrroles from Streptomyces rimosus with bacterial protein histidine kinase inhibitory and antimicrobial activities

机译：来自链霉菌的新型链霉素，具有细菌蛋白组氨酸激酶抑制和抗菌活性

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摘要

A series of halogenated pyrrolo [2,1-b] [1,3] benzoxazines (1 similar to 9) was isolated from fermentations of an actinomycete strain X10/78/978 (NCIMB40808), identified as Streptomyces rimosus, during a microbial extract screening programme to identify inhibitors of bacterial histidine kinase. The structures of these compounds were elucidated by spectroscopic methods including the HMQC, HMBC and INADEQUATE NMR experiments. The structure of 1 was confirmed by X-ray crystallographic studies. Compounds 5 and 6 were produced in fermentations in the presence of NaBr and NaI respectively. The most abundant member of the series, streptopyrrole, 1, inhibited the nitrogen regulator II (NRII) histidine kinase from Escherichia roll with an IC50 of 20 mu M and exhibited antimicrobial activity against a range of bacteria and fungi. [References: 16]
机译：从微生物提取物中的放线菌菌株X10 / 78/978（NCIMB40808）的发酵中分离出一系列卤代吡咯并[2,1-b] [1,3]苯并恶嗪（1与9类似）。筛选程序以鉴定细菌组氨酸激酶的抑制剂。通过包括HMQC，HMBC和INADEQUATE NMR实验在内的光谱方法阐明了这些化合物的结构。 1的结构通过X射线晶体学研究确认。化合物5和6分别在NaBr和NaI存在下发酵产生。该系列中最丰富的成员链霉菌戊酮1抑制了大肠埃希氏菌中的氮调节剂II（NRII）组氨酸激酶，IC50为20μM，并且对多种细菌和真菌表现出抗菌活性。 [参考：16]

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