Mechanism of action of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the causative agent of Chagas' disease.
نویسندگان
چکیده
We investigated the molecular basis of the activity of 4-phenoxyphenoxyethyl thiocyanate (WC-9) against Trypanosoma cruzi, the etiological agent of Chagas' disease. We found that growth inhibition of T. cruzi epimastigotes induced by this compound was associated with a reduction in the content of the parasite's endogenous sterols due to a specific blockade of their de novo synthesis at the level of squalene synthase.
منابع مشابه
Fluorine-containing aryloxyethyl thiocyanate derivatives are potent inhibitors of Trypanosoma cruzi and Toxoplasma gondii proliferation.
As a part of our project aimed at developing new safe chemotherapeutic and chemoprophylactic agents against tropical diseases, fluorine-containing drugs structurally related to 4-phenoxyphenoxyethyl thiocyanate (1) were designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible of American trypanosomiasis (Chagas' disease), and Toxoplasm...
متن کاملDesign and synthesis of aryloxyethyl thiocyanate derivatives as potent inhibitors of Trypanosoma cruzi proliferation.
As a part of our project directed at the search of new chemotherapeutic agents against American trypanosomiasis (Chagas' disease), several drugs possessing the 4-phenoxyphenoxy skeleton and other closely related structures employing the thiocyanate moiety as polar end group were designed, synthesized, and evaluated as antiproliferative agents against Trypanosoma cruzi, the parasite responsible ...
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 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 کاملSqualene Synthase As a Target for Chagas Disease Therapeutics
Trypanosomatid parasites are the causative agents of many neglected tropical diseases and there is currently considerable interest in targeting endogenous sterol biosynthesis in these organisms as a route to the development of novel anti-infective drugs. Here, we report the first x-ray crystallographic structures of the enzyme squalene synthase (SQS) from a trypanosomatid parasite, Trypanosoma ...
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ورودعنوان ژورنال:
- Antimicrobial agents and chemotherapy
دوره 47 6 شماره
صفحات -
تاریخ انتشار 2003