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Future Med Chem ; 10(8): 863-878, 2018 04 01.
Article in English | MEDLINE | ID: mdl-29589477

ABSTRACT

AIM: Metronidazole is the most widely used drug in trichomoniasis therapy. However, the emergence of metronidazole-resistant Trichomonas vaginalis isolates calls for the search for new drugs to counter the pathogenicity of these parasites. RESULTS: Classification models for predicting the antitrichomonas activity of molecules were built. These models were employed to screen antiprotozoal drugs, from which 20 were classified as active. The in vitro experiments showed moderate to high activity for 19 of the molecules at 10 µg/ml, while 3 compounds yielded higher activity than the reference at 1 µg/ml. The 11 most active chemicals were evaluated in vivo using Naval Medical Research Institute (NMRI) mice. CONCLUSION: Benznidazole showed similar results as metronidazole, and can thus be considered as a potential candidate in antitrichomonas therapy.


Subject(s)
Antiprotozoal Agents/chemistry , Antiprotozoal Agents/pharmacology , Drug Repositioning/methods , Trichomonas Infections/drug therapy , Trichomonas vaginalis/drug effects , Animals , Antiprotozoal Agents/therapeutic use , Discriminant Analysis , Drug Resistance , Female , Humans , Metronidazole/chemistry , Metronidazole/pharmacology , Metronidazole/therapeutic use , Mice , Nitroimidazoles/chemistry , Nitroimidazoles/pharmacology , Nitroimidazoles/therapeutic use , Trichomonas Vaginitis/drug therapy
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