Drug repositioning for novel antitrichomonas from known antiprotozoan drugs using hierarchical screening

Future Medicinal Chemistry
Alfredo Meneses-MarcelVicente J Arán-Redó


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. 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. Benznidazole showed similar results as metronidazole, and can thus be considered as a potential candidate in antitrichomonas therapy.


Jun 1, 1975·The Journal of Antimicrobial Chemotherapy·Y Buchner, D I Edwards
Feb 1, 1975·Parasitology·L P Joyner, C C Norton
May 1, 1996·Antimicrobial Agents and Chemotherapy·E M Narcisi, W Evan Secor
Feb 1, 1996·Journal of Veterinary Pharmacology and Therapeutics·S InghelbrechtJ Vercruysse
Jun 1, 1997·Parasite : Journal De La Société Française De Parasitologie·J J Nogal RuizAlicia Gómez Barrio
Jul 25, 2000·Journal of Ethnopharmacology·S Muelas-SerranoAlicia Gómez-Barrio
Dec 26, 2001·The Journal of Antimicrobial Chemotherapy·I Sullayman AdaguJean-François Rossignol
Jul 18, 2002·The Journal of Eukaryotic Microbiology·Roberto Cedillo-RiveraLilian Yépez-Mulia
Dec 21, 2002·Lancet·Michel A MissinouPeter G Kremsner
Feb 28, 2003·Journal of Health Economics·Joseph A DiMasiHenry G Grabowski
Mar 5, 2003·The Lancet Infectious Diseases·Trudie Lang, Brian Greenwood
Sep 17, 2003·Cell Research·Rebecca L DunneJacqueline A Upcroft
Sep 1, 1960·The British Journal of Venereal Diseases·P DURELC GIROT
Mar 1, 1965·Poultry Science·C A JOHNSON, J O'CONNOR
Oct 15, 2003·Bioorganic & Medicinal Chemistry·Man-Chin ChungElizabeth Igne Ferreira
Dec 12, 2003·Nature Reviews. Drug Discovery·Solomon Nwaka, Robert G Ridley
Nov 24, 2005·Antimicrobial Agents and Chemotherapy·Ivan HrdýJan Tachezy
Feb 4, 2006·Bioorganic & Medicinal Chemistry Letters·María Celeste VegaF Torrens
Feb 28, 2006·Revista Da Sociedade Brasileira De Medicina Tropical·Marcelo Corti, Claudio Yampolsky
Mar 9, 2006·Health Affairs·Christopher P Adams, Van V Brantner
Apr 12, 2006·CMAJ : Canadian Medical Association Journal = Journal De L'Association Medicale Canadienne·Erica Weir
Apr 22, 2006·Comparative Biochemistry and Physiology. Part A, Molecular & Integrative Physiology·Juan Diego MayaAntonio Morello
Aug 10, 2007·Nature·Curtis R Chong, David J Sullivan
Apr 12, 2008·Clinical Neuropathology·P M Foye
May 17, 2008·Journal of Computer-aided Molecular Design·Yovani Marrero-PonceVicente J Arán
Aug 30, 2008·Journal of Biomolecular Screening·Alfredo Meneses-MarcelVicente J Arán
Feb 12, 2009·European Journal of Medicinal Chemistry·Emanuel Hernández-NúñezGabriel Navarrete-Vazquez
Oct 27, 2009·European Journal of Pharmaceutical Sciences : Official Journal of the European Federation for Pharmaceutical Sciences·Juan Alberto Castillo-GaritFacundo Pérez-Giménez
Jan 14, 2010·Clinical Infectious Diseases : an Official Publication of the Infectious Diseases Society of America·Sonja LöfmarkCarl Erik Nord
Nov 1, 2011·Antimicrobial Agents and Chemotherapy·Belinda S Hall, Shane R Wilkinson
Oct 17, 2012·SAR and QSAR in Environmental Research·Stephen J BarigyeJ Galvez
Jun 25, 2013·Sexually Transmitted Infections·E Brook Goodhew, W Evan Secor
Jan 2, 2014·Pharmacological Reviews·Gregory SliwoskiEdward W Lowe
Jun 4, 2014·Journal of Computational Chemistry·César R García-JacasErnesto Contreras-Torres
Aug 12, 2014·Journal of Microbiological Methods·Alexandra Ibáñez-EscribanoJosé Antonio Escario
Apr 16, 2017·BMC Veterinary Research·David LoveJames A Thompson


Jun 5, 2020·Expert Opinion on Drug Discovery·Riccardo ZanniJ Galvez

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