The total synthesis of norfijimycin A, a simplified analogue of the marine natural product fijimycin A, is described. Fijimycin A is a cyclic depsipeptide that has been shown to possess activity against methicillin-resistant Staphylococcus aureus. The natural product contains a rare N,β-dimethyl leucine unit with unknown stereochemistry at the β-carbon. To evaluate the importance of the β-methyl group for antimicrobial activity, we introduced N-methyl leucine into the natural product scaffold. The resulting norfijimycin A was shown to possess significant activity against Mycobacterium tuberculosis, the etiological agent of tuberculosis.

中文翻译：

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具有抗结核分枝杆菌活性的诺非霉素A的合成

描述了海洋天然产物斐济霉素A的简化类似物诺非霉素A的全合成。斐济霉素A是一种环状二肽，已显示对耐甲氧西林的金黄色葡萄球菌具有活性。天然产物含有罕见的N，β-二甲基亮氨酸单元，在β-碳上的立体化学未知。为了评估β-甲基对抗菌活性的重要性，我们将N-甲基亮氨酸引入了天然产物支架中。所得的诺非霉素A显示出对结核分枝杆菌（结核分枝杆菌）具有显着的活性。