|
|||||
|
|
Synthesis of benzologues of Nitazoxanide and Tizoxanide: a comparative study of their in vitro broad-spectrum antiprotozoal activity |
|
| Authors: | Navarrete-Vazquez Gabriel Chávez-Silva Fabiola Argotte-Ramos Rocío Rodríguez-Gutiérrez María del Carmen Chan-Bacab Manuel Jesús Cedillo-Rivera Roberto Moo-Puc Rosa Hernández-Nuñez Emanuel |
| Institution: | a Facultad de Farmacia, Universidad Autónoma del Estado de Morelos, Cuernavaca, Morelos 62209, Mexico b Centro de Investigación sobre Enfermedades Infecciosas, Instituto Nacional de Salud Pública, Cuernavaca, Morelos 62508, Mexico c Departamento de Microbiología Ambiental y Biotecnología, Universidad Autónoma de Campeche, Campeche 24030, Mexico d Unidad de Investigación Médica Yucatán, IMSS Mérida, Yucatán 97000, Mexico e Facultad de Química, Universidad Autónoma de Yucatán, Mérida, Yucatán 97000, Mexico |
| Abstract: | 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 IC50’s <5μM. 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. |
| Keywords: | Nitazoxanide Giardia intestinalis Leishmania mexicana Benzologue |
| 本文献已被 ScienceDirect PubMed 等数据库收录！ | |