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首页> 外文期刊>The Journal of Antibiotics: An International Journal >Thiazomycin, nocathiacin and analogs show strong activity against clinical strains of drug-resistant Mycobacterium tuberculosis
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Thiazomycin, nocathiacin and analogs show strong activity against clinical strains of drug-resistant Mycobacterium tuberculosis

机译：噻嗪霉素，NocathiaNin和类似物表现出强烈的抗药性结核病患者抗药性抗药性菌株

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摘要

Thiazolyl peptides are a class of natural products with potent Gram-positive antibacterial activities. Lack of aqueous solubility precluded this class of compounds from advancing to clinical evaluations. Nocathiacins and thiazomycins are sub-classes of thiazolyl peptides that are endowed with structural features amenable for chemical modifications. Semi-synthetic modifications of nocathiacin led to a series of analogs with improved water solubility, while retaining potency and antibacterial spectrum. We studied the activities of a selection of two natural products (nocathiacin and thiazomycin) as well as seven polar semi-synthetic analogs against twenty clinical strains of Mycobacterium tuberculosis with MDR phenotypes. Two compounds show useful activity against H37Rv strain with MIC values <= 1 mu M, two (<= 0.5 mu M) and three (<= 10 mu M). These two derivatives showed MIC values <= 2.5 mu M against most of the 20 MDR strains regardless their resistance profile. Specifically, these lack cross-resistance to rifampicin, isoniazid and moxifloxacin.
机译：噻唑酯肽是一类天然产物，具有有效的革兰氏阳性抗菌活性。缺乏含水溶解度迫使这类化合物推进到临床评价。 NocathiaCins和噻唑胺是噻唑基肽的亚类亚唑肽，其赋予结构特征，适用于化学修饰。 NocathiaN的半合成修饰导致了一系列的类似水溶性的类似物，同时保持效力和抗菌谱。我们研究了各种两种天然产物（NocathiaCin和噻嗪霉素）的活动以及七种极性半合成模拟与MDR表型对抗二十个分枝杆菌的结核病菌株。两种化合物显示出对H37RV菌株的有用活性，MIC值<=1μm，两（<=0.5μm）和三（<=10μm）。这两个衍生物显示出麦克风值<=2.5μm，与它们的电阻曲线无关。具体而言，这些缺乏对利福平，异烟肼和Moxifloxacin的交叉抗性。

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