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Comparative Study of Activities of a Diverse Set of Antimycobacterial Agents against Mycobacterium tuberculosis and Mycobacterium ulcerans

机译:一套不同的分枝杆菌药抗结核分枝杆菌和溃疡分枝杆菌活性的比较研究

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摘要

A library of compounds covering a broad chemical space was selected from a tuberculosis drug development program and was screened in a whole-cell assay against Mycobacterium ulcerans, the causative agent of the necrotizing skin disease Buruli ulcer. While a number of potent antitubercular agents were only weakly active or inactive against M. ulcerans, five compounds showed high activity (90% inhibitory concentration [IC90], ≤1 μM), making screening of focused antitubercular libraries a good starting point for lead generation against M. ulcerans.
机译:从结核药物开发计划中选择了涵盖广泛化学空间的化合物库,并在全细胞测定中筛选了针对坏死性皮肤病布鲁氏菌病致病菌溃疡分枝杆菌的全细胞方法。尽管许多有效的抗结核药物对溃疡分支杆菌均具有弱活性或无活性,但五种化合物显示出高活性(抑制浓度为90%[IC90],≤1μM),这使筛选集中的抗结核文库成为了产生铅的良好起点针对溃疡分枝杆菌。

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