抗细菌
噻唑
异源表达
立体化学
喹啉
部分
基因簇
异源的
链霉菌
化学
生物
计算生物学
生物化学
结核分枝杆菌
遗传学
细菌
重组DNA
基因
有机化学
医学
肺结核
病理
作者
Wei Liu,Shilan Zhai,Liping Zhang,Yuchan Chen,Zhiyong Liu,Wanli Ma,Tianyu Zhang,Weimin Zhang,Liang Ma,Changsheng Zhang,Wenjun Zhang
标识
DOI:10.1021/acs.jnatprod.3c01132
摘要
Thiazole scaffold-based small molecules exhibit a range of biological activities and play important roles in drug discovery. Based on bioinformatics analysis, a putative biosynthetic gene cluster (BGC) for thiazole-containing compounds was identified from Streptomyces sp. SCSIO 40020. Heterologous expression of this BGC led to the production of eight new thiazole-containing compounds, grisechelins E, F, and I–N (1, 2, 5–10), and two quinoline derivatives, grisechelins G and H (3 and 4). The structures of 1–10, including their absolute configurations, were elucidated by HRESIMS, NMR spectroscopic data, ECD calculations, and single-crystal X-ray diffraction analysis. Grisechelin F (2) is a unique derivative, distinguished by the presence of a salicylic acid moiety. The biosynthetic pathway for 2 was proposed based on bioinformatics analysis and in vivo gene knockout experiments. Grisechelin E (1) displayed moderate antimycobacterial activity against Mycobacterium tuberculosis H37Ra (MIC of 8 μg mL–1).
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