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新型结核病药物问世在望。

New tuberculosis drugs on the horizon.

机构信息

Global Health Institute, Ecole Polytechnique Fédérale de Lausanne, CH-1015 Lausanne, Switzerland.

出版信息

Curr Opin Microbiol. 2011 Oct;14(5):570-6. doi: 10.1016/j.mib.2011.07.022. Epub 2011 Aug 5.

Abstract

Tuberculosis (TB) remains a major global health concern whose control has been exacerbated by HIV and the emergence of multidrug-resistant (MDR-TB) and extensively drug-resistant (XDR-TB) strains of Mycobacterium tuberculosis. The demand for new and faster acting TB drugs is thus greater than ever. In the past decade intensive efforts have been made to discover new leads for TB drug development using both target-based and cell-based approaches. Here, we describe the most promising anti-tubercular drug candidates that are in clinical development and introduce some nitro-aromatic compounds that inhibit a new target, DprE1, an essential enzyme involved in a crucial step in mycobacterial cell wall biosynthesis.

摘要

结核病(TB)仍然是一个主要的全球健康关注点,其控制因 HIV 以及耐多药(MDR-TB)和广泛耐药(XDR-TB)结核分枝杆菌菌株的出现而变得更加复杂。因此,对新型和更快速作用的 TB 药物的需求比以往任何时候都更加迫切。在过去的十年中,人们已经做出了巨大的努力,通过基于靶点和基于细胞的方法,来发现新的 TB 药物开发的先导化合物。在这里,我们描述了一些处于临床开发阶段的最有前途的抗结核候选药物,并介绍了一些抑制新靶点 DprE1 的硝基芳香族化合物,该靶点是分枝杆菌细胞壁生物合成中关键步骤所必需的酶。

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