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抗结核药物研发的当前进展:强效原型与新靶点

Current Advances in Antitubercular Drug Discovery: Potent Prototypes and New Targets.

作者信息

Dos Santos Fernandes Guilherme Felipe, Jornada Daniela Hartmann, de Souza Paula Carolina, Chin Chung Man, Pavan Fernando Rogerio, Dos Santos Jean Leandro

机构信息

School of Pharmaceutical Sciences, State University of Sao Paulo, Zipcode: 14801- 902, Araraquara, Brazil.

出版信息

Curr Med Chem. 2015;22(27):3133-61. doi: 10.2174/0929867322666150818103836.

Abstract

Tuberculosis (TB) is an infectious disease caused by bacterium of the Mycobacterium genus, mainly by Mycobacterium tuberculosis (MTB). The World Health Organization aims to substantially reduce the number of cases in the coming years; however, the increased number of multidrug-resistant (MDR) and extremely drug-resistant (XDR) forms of the bacterium and the lack of treatment for latent tuberculosis are challenges to be overcome. In this review, we have identified the most potent compounds described in the literature during recent years with MIC values < 7 µM, low toxicity and a high selective index. In addition, emerging targets in MTB are presented to provide new perspectives for the discovery of new antitubercular drugs. This review aims to summarize the current advances in and promote insights into antitubercular drug discovery.

摘要

结核病(TB)是一种由分枝杆菌属细菌引起的传染病,主要由结核分枝杆菌(MTB)引起。世界卫生组织旨在在未来几年大幅减少病例数量;然而,该细菌耐多药(MDR)和广泛耐药(XDR)形式数量的增加以及潜伏性结核病缺乏治疗方法是有待克服的挑战。在本综述中,我们确定了近年来文献中描述的最有效的化合物,其最低抑菌浓度(MIC)值<7 μM,毒性低且选择性指数高。此外,还介绍了MTB中的新靶点,为发现新型抗结核药物提供新的视角。本综述旨在总结抗结核药物发现的当前进展并促进对其的深入了解。

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