Evaluating Aziridinyl Nitrobenzamide Compounds as Leishmanicidal Prodrugs
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چکیده
منابع مشابه
Evaluating aziridinyl nitrobenzamide compounds as leishmanicidal prodrugs.
Many of the nitroaromatic agents used in medicine function as prodrugs and must undergo activation before exerting their toxic effects. In most cases, this is catalyzed by flavin mononucleotide (FMN)-dependent type I nitroreductases (NTRs), a class of enzyme absent from higher eukaryotes but expressed by bacteria and several eukaryotic microbes, including trypanosomes and Leishmania. Here, we u...
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Nitroaromatic prodrugs are used to treat a range of microbial infections with selectivity achieved by specific activation reactions. For trypanosomatid parasites, this is mediated by type I nitroreductases. Here, we demonstrate that the causative agent of leishmaniasis, Leishmania major, expresses an FMN-containing nitroreductase (LmNTR) that metabolizes a wide range of substrates, and based on...
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 2013
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.01459-13