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

Authors :
Alexandra Ibáñez-Escribano
César R. García-Jacas
Yanetsy Machado-Tugores
Alfredo Meneses-Marcel
Juan José Nogal-Ruiz
Vicente J Arán-Redó
Stephen J. Barigye
Enrique Teran
Yovani Marrero-Ponce
Alicia Gómez-Barrio
José Antonio Escario
Source :
Digital.CSIC. Repositorio Institucional del CSIC, instname
Publication Year :
2018

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.

Details

ISSN :
17568927
Volume :
10
Issue :
8
Database :
OpenAIRE
Journal :
Future medicinal chemistry
Accession number :
edsair.doi.dedup.....da738f327f15ba2a1180d7cb73e46074