Trypanocidal Activity of Aziridinyl Nitrobenzamide Prodrugs
نویسندگان
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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Quinone-based compounds have been exploited to treat infectious diseases and cancer, with such chemicals often functioning as inhibitors of key metabolic pathways or as prodrugs. Here, we screened an aziridinyl 1,4-benzoquinone (ABQ) library against the causative agents of trypanosomiasis, and cutaneous leishmaniasis, identifying several potent structures that exhibited EC50 values of <100 nM. ...
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Trypanosoma cruzi, a hemoflagellate protozoan (family Trypanosomatidae), is the ethiological agent of Chagas disease, which is affecting 16-18 million people, with more than 100 million exposed to the risk of infection. Higher plants are a potential source of new drugs to improve the treatment of Chagase disease. Until recently, Rutacea, Meliaceae, Simaroubaceae and Burceraceae families have be...
متن کاملTrypanocidal activity of some endemic species of Satureja in Iran
Trypanosoma cruzi, a hemoflagellate protozoan (family Trypanosomatidae), is the ethiological agent of Chagas disease, which is affecting 16-18 million people, with more than 100 million exposed to the risk of infection. Higher plants are a potential source of new drugs to improve the treatment of Chagase disease. Until recently, Rutacea, Meliaceae, Simaroubaceae and Burceraceae families have be...
متن کاملThe trypanocidal activity of naphthoquinones: a review.
Naphthoquinones are compounds present in several families of higher plants. Their molecular structures confer redox properties, and they are involved in multiple biological oxidative processes. In folk medicine, especially among Indian populations, plants containing naphthoquinones have been employed for the treatment of various diseases. The biological redox cycle of quinones can be initiated ...
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ژورنال
عنوان ژورنال: Antimicrobial Agents and Chemotherapy
سال: 2010
ISSN: 0066-4804,1098-6596
DOI: 10.1128/aac.00800-10