Synthesis and antiprotozoal activity of nitazoxanideaN-methylbenzimidazole hybrids

A series of a novel hybrid compounds between nitazoxanide and N-methylbenzimidazole were synthesized starting from the corresponding N-methyl-2-nitroanilines. The new hybrid compounds (1a13) were evaluated in vitro against Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis. NTZ, MTZ...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2013-12, Vol.23 (24), p.6838-6841
Hauptverfasser: Soria-Arteche, Olivia, Hernandez-Campos, Alicia, Yepez-Mulia, LiliA!n, Trejo-Soto, Pedro, Hernandez-Luis, Francisco, Gres-Molina, Jorge, Maldonado, Luis, Castillo, Rafael
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Sprache:eng
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Zusammenfassung:A series of a novel hybrid compounds between nitazoxanide and N-methylbenzimidazole were synthesized starting from the corresponding N-methyl-2-nitroanilines. The new hybrid compounds (1a13) were evaluated in vitro against Giardia intestinalis, Entamoeba histolytica, Trichomonas vaginalis. NTZ, MTZ and ABZ were used as drug standards. Experimental evaluations revealed all of the new compounds (1a13) were active and showed strong activity against the three protozoa, particularly with E. histolytica where the IC50 values ranged between 3 and 69 nM.
ISSN:0960-894X
DOI:10.1016/j.bmcl.2013.10.011