Synthesis and antiprotozoal activity of nitazoxanide-N-methylbenzimidazole hybrids
Olivia Soria-Arteche1, Alicia Hernández-Campos, Lilián Yépez-Mulia
1Departamento de Sistemas Biológicos, División Ciencias Biológicas y de la Salud, UAM-Xochimilco, México, DF 04960, Mexico; Facultad de Química, Departamento de Farmacia, UNAM, México, DF 04510, Mexico.
Abstract:
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 (1-13) 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 (1-13) were active and showed strong activity against the three protozoa, particularly with E. histolytica where the IC50 values ranged between 3 and 69 nM. Overall, compounds 2, 5, 7, 8, 9, 11 and 12 stood out with values lower than 87 nM for all three protozoa, comparatively better than the reference drugs.
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