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对复制期和休眠期结核分枝杆菌均有活性的新型1-羟基-2-硫代吡啶衍生物。

New 1-hydroxy-2-thiopyridine derivatives active against both replicating and dormant Mycobacterium tuberculosis.

作者信息

Salina Elena G, Ryabova Olga, Vocat Anthony, Nikonenko Boris, Cole Stewart T, Makarov Vadim

机构信息

Bach Institute of Biochemistry, Research Center of Biotechnology of the Russian Academy of Sciences, Moscow, Russia.

Bach Institute of Biochemistry, Research Center of Biotechnology of the Russian Academy of Sciences, Moscow, Russia.

出版信息

J Infect Chemother. 2017 Nov;23(11):794-797. doi: 10.1016/j.jiac.2017.04.012. Epub 2017 May 18.

Abstract

Tuberculosis (TB) treatment is confounded by the range of metabolic states displayed by Mycobacterium tuberculosis, by the long duration required and by the increasing prevalence of drug-resistant strains. Latent TB infection is especially difficult to treat due to the phenotypic antibiotic resistance of non-replicating M. tuberculosis. Therefore, the development of new drugs effective against both active and latent TB infection is needed. New 1-hydroxy-2-thiopyridine derivatives were synthesized and found to be highly effective in vitro against both actively growing and dormant non-culturable M. tuberculosis. Such compounds are leads for the development of new drugs for all forms of TB including latent infection.

摘要

结核病(TB)的治疗因结核分枝杆菌所呈现的一系列代谢状态、所需的漫长疗程以及耐药菌株患病率的不断上升而变得复杂。潜伏性结核感染尤其难以治疗,因为非复制型结核分枝杆菌具有表型抗生素耐药性。因此,需要开发对活动性和潜伏性结核感染均有效的新药。合成了新型1-羟基-2-硫代吡啶衍生物,发现其在体外对活跃生长和休眠的不可培养结核分枝杆菌均具有高效。此类化合物是开发针对包括潜伏感染在内的所有形式结核病新药的先导物。

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