Mechanism of Action of 5-Nitrothiophenes against Mycobacterium tuberculosis

被引：28

作者：

Hartkoorn, Ruben C. ^{[1
]}

Ryabova, Olga B. ^{[2
]}

Chiarelli, Laurent R. ^{[3
]}

Riccardi, Giovanna ^{[3
]}

Makarov, Vadim ^{[2
]}

Cole, Stewart T. ^{[1
]}

机构：

[1] Ecole Polytech Fed Lausanne, Global Hlth Inst, Lausanne, Switzerland

[2] Russian Acad Sci, AN Bakh Biochem Inst, Moscow, Russia

[3] Univ Pavia, Dipartimento Biol & Biotecnol, I-27100 Pavia, Italy

来源：

ANTIMICROBIAL AGENTS AND CHEMOTHERAPY | 2014年 / 58卷 / 05期

关键词：

COENZYME F-420; BOVIS BCG; BIOSYNTHESIS; DISCOVERY; CANDIDATE; DRUGS; ASSAY;

D O I：

10.1128/AAC.02693-13

中图分类号：

Q93 [微生物学];

学科分类号：

071005 ; 100705 ;

摘要：

On using the streptomycin-starved 18b strain as a model for nonreplicating Mycobacterium tuberculosis, we identified a 5-nitrothiophene compound as highly active but not cytotoxic. Mutants resistant to 5-nitrothiophenes were found be cross-resistant to the nitroimidazole PA-824 and unable to produce the F-420 cofactor. Furthermore, 5-nitrothiophenes were shown to be activated by the F-420-dependent nitroreductase Ddn and to release nitric oxide, a mechanism of action identical to that described for nitroimidazoles.

引用

页码：2944 / 2947

页数：4

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