Antischistosomal versus Antiandrogenic Properties of Aryl Hydantoin Ro 13-3978
نویسندگان
چکیده
منابع مشابه
Aryl hydantoin Ro 13-3978, a broad-spectrum antischistosomal.
OBJECTIVES Praziquantel is the only drug available for the treatment of schistosomiasis and the state of the exhausted drug discovery pipeline is alarming. We restarted investigations on the abandoned antischistosomal Ro 13-3978, an aryl hydantoin discovered in the early 1980s by Hoffmann La-Roche. METHODS Newly transformed schistosomula and adult Schistosoma mansoni were studied in the prese...
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The aryl hydantoin 1 (Ro 13-3978) was identified in the early 1980s as a promising antischistosomal lead compound. However, this series of aryl hydantoins produced antiandrogenic side effects in the host, a not unexpected outcome given their close structural similarity to the antiandrogenic drug nilutamide. Building on the known SAR of this compound series, we now describe a number of analogs o...
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BACKGROUND The treatment and control of schistosomiasis, an often neglected tropical disease that exacerbates poverty, depends on a single drug, praziquantel. The large-scale use of praziquantel might select for drug-resistant parasites, hence there is a need to develop new antischistosomal compounds. Here, we report that the antimalarial drug mefloquine possesses promising antischistosomal pro...
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ژورنال
عنوان ژورنال: The American Journal of Tropical Medicine and Hygiene
سال: 2014
ISSN: 0002-9637,1476-1645
DOI: 10.4269/ajtmh.14-0029