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Synthesis of benzologues of Nitazoxanide and Tizoxanide: A comparative study of their in vitro broad-spectrum antiprotozoal activity by Gabriel Navarrete-Vazquez; Fabiola Chávez-Silva; Rocío Argotte-Ramos; María del Carmen Rodríguez-Gutiérrez; Manuel Jesús Chan-Bacab; Roberto Cedillo-Rivera; Rosa Moo-Puc; Emanuel Hernández-Nuñez is a Biochemistry, Genetics and Molecular Biology article available to read on EtoBox.

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We have synthesized two new benzologues of Nitazoxanide (NIT) and Tizoxanide (TIZ), using a short synthetic route. Both compounds were tested in vitro against six protozoa (Giardia intestinalis, Trichomonas vaginalis, Entamoeba histolytica, Plasmodium berghei, Leishmania mexicana and Trypanosoma cruzi). Compound 1 (benzologue of NIT) showed broad antiprotozoal effect against all parasites tested, showing IC 50 's <5lM. This compound was five-times more active than NIT, and 18-times more potent than metronidazole against G. intestinalis. It was 10-times more active than pentamidine against L. mexicana, and it was sevenfold more potent than benznidazole versus T. cruzi. This compound could be considered as a new broad spectrum antiprotozoal agent.

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Author

Gabriel Navarrete-Vazquez; Fabiola Chávez-Silva; Rocío Argotte-Ramos; María del Carmen Rodríguez-Gutiérrez; Manuel Jesús Chan-Bacab; Roberto Cedillo-Rivera; Rosa Moo-Puc; Emanuel Hernández-Nuñez

Publisher

Elsevier Science; Elsevier ; Elsevier Ltd.; Elsevier BV (ISSN 0960-894X)

Published

2011

Language

EN

Field

Biochemistry, Genetics and Molecular Biology (Life Sciences)