期刊
ANGEWANDTE CHEMIE-INTERNATIONAL EDITION
卷 53, 期 52, 页码 14605-14609出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/anie.201409964
关键词
antibiotics; myxobacteria; natural products; NRPS; topoisomerase inhibitors
The development of new antibiotics faces a severe crisis inter alia owing to a lack of innovative chemical scaffolds with activities against Gram-negative and multiresistant pathogens. Herein, we report highly potent novel antibacterial compounds, the myxobacteria-derived cystobactamids 1-3, which were isolated from Cystobacter sp. and show minimum inhibitory concentrations in the low mu gmL(-1) range. We describe the isolation and structure elucidation of three congeners as well as the identification and annotation of their biosynthetic gene cluster. By studying the self-resistance mechanism in the natural producer organism, the molecular targets were identified as bacterial type IIa topoisomerases. As quinolones are largely exhausted as a template for new type II topoisomerase inhibitors, the cystobactamids offer exciting alternatives to generate novel antibiotics using medicinal chemistry and biosynthetic engineering.
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