PDF(Pubmed)
Abstract：
The aim of this study was to obtain new halolactones with a gem-dimethyl group in the cyclohexane ring (at the C-3 or C-5 carbon) and a methyl group in the lactone ring and then subject them to biotransformations using filamentous fungi. Halolactones in the form of mixtures of two diasteroisomers were subjected to screening biotransformations, which showed that only compounds with a gem-dimethyl group located at the C-5 carbon were transformed. Strains from the genus Fusarium carried out hydrolytic dehalogenation, while strains from the genus Absidia carried out hydroxylation of the C-7 carbon. Both substrates and biotransformation products were then tested for antimicrobial activity against multidrug-resistant strains of both bacteria and yeast-like fungi. The highest antifungal activity against C. dubliniensis and C. albicans strains was obtained for compound 5b, while antimicrobial activity against S. aureus MRSA was obtained for compound 4a.
摘要：
这项研究的目的是获得新的卤代内酯，其在环己烷环（在C-3或C-5碳）中具有宝石-二甲基基团，在内酯环中具有甲基基团，然后使用丝状真菌对其进行生物转化。对两种非对映异构体混合物形式的卤代内酯进行生物转化筛选，这表明只有具有位于C-5碳的宝石-二甲基基团的化合物被转化。镰刀菌属菌株进行水解脱卤，而来自Absidia属的菌株对C-7碳进行了羟基化。然后测试底物和生物转化产物对细菌和酵母样真菌的多重耐药菌株的抗微生物活性。化合物5b对杜布立尼和白色念珠菌的抗真菌活性最高，而化合物4a获得了对金黄色葡萄球菌MRSA的抗微生物活性。
