Synthesis and antiprotozoal activity of nitazoxanide-N-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 (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.
['Soria-Arteche|Olivia|O|', 'Hernández-Campos|Alicia|A|', 'Yépez-Mulia|Lilián|L|', 'Trejo-Soto|Pedro Josué|PJ|', 'Hernández-Luis|Francisco|F|', 'Gres-Molina|Jorge|J|', 'Maldonado|Luis A|LA|', 'Castillo|Rafael|R|']
D000981:Antiprotozoal Agents D001562:Benzimidazoles D015195:Drug Design D004748:Entamoeba histolytica D056890:Eukaryota D016829:Giardia lamblia D009574:Nitro Compounds D013844:Thiazoles D014246:Trichomonas vaginalis
Hybrid compounds Nitazoxanide Giardia intestinalis Entamoeba histolytica Trichomonas vaginalis Benzimidazole