VII Simposio Internacional de Ciencias Farmacéuticas 2019 "VII SICF" -VII Simposio "Diseño, Obtención y Desarrollo de Fármacos"

VII Simposio Internacional de Ciencias Farmacéuticas 2019

VII SICF

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

Resumen

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. Classifiation models for predicting the antitrichomonas activity of molecules were built. These models were employed to screen antiprotozoal drugs, from which 20 were classifid 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.

Abstract

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. Classifiation models for predicting the antitrichomonas activity of molecules were built. These models were employed to screen antiprotozoal drugs, from which 20 were classifid 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.

Sobre el ponente

Alfredo Meneses Marcel

Dr. Alfredo Meneses Marcel

Centro de Bioactivos Químicos Flag of Cuba
Información Práctica
Póster digital
Spanish / Español
No definido
30 minutos
No definido
Autores
Yanetsy Machado Tugores
Alicia Gomez Barrio
Vicente Arán Redó
Jose A Escario
Cesar R García Jacas
Dr. Alfredo Meneses Marcel
Stephen J Barigye
Yovani Marrero Ponce
Juan J Nogal Ruiz
Enrique Teran
Alexandra Ibáñez Escribano
Palabras clave
in vitro
in vivo
qsar
trichomonas vaginalis
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