Synthesis of benzologues of Nitazoxanide and Tizoxanide: A comparative study of their in vitro broad-spectrum antiprotozoal activity

被引：44

作者：

Navarrete-Vazquez, Gabriel ^{[1
]}

Chavez-Silva, Fabiola ^{[1
]}

Argotte-Ramos, Rocio ^{[2
]}

del Carmen Rodriguez-Gutierrez, Maria ^{[2
]}

Jesus Chan-Bacab, Manuel ^{[3
]}

Cedillo-Rivera, Roberto ^{[4
]}

Moo-Puc, Rosa ^{[4
]}

Hernandez-Nunez, Emanuel ^{[1
,5
]}

机构：

[1] Univ Autonoma Estado Morelos, Fac Farm, Cuernavaca 62209, Morelos, Mexico

[2] Inst Nacl Salud Publ, Ctr Invest Enfermedades Infecciosas, Cuernavaca 62508, Morelos, Mexico

[3] Univ Autonoma Campeche, Dept Microbiol Ambiental & Biotecnol, Campeche 24030, Mexico

[4] IMSS Merida, Unidad Invest Med Yucatan, Yucaton 97000, Mexico

[5] Univ Autonoma Yucatan Merida, Fac Quim, Merida 97000, Yucatan, Mexico

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2011年 / 21卷 / 10期

关键词：

Nitazoxanide; Giardia intestinalis; Leishmania mexicana; Benzologue; PLASMODIUM-BERGHEI; DESIGN; PARASITES;

D O I：

10.1016/j.bmcl.2011.02.100

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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 <5 mu M. 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. (C) 2011 Elsevier Ltd. All rights reserved.

引用

页码：3168 / 3171

页数：4

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