Synthesis and antiprotozoal activity of nitazoxanide-N-methylbenzimidazole hybrids
| Autor: | Olivia Soria-Arteche, Jorge Gres-Molina, Lilián Yépez-Mulia, Pedro Josué Trejo-Soto, Francisco Hernández-Luis, Alicia Hernández-Campos, Rafael Castillo, Luis A. Maldonado |
|---|---|
| Rok vydání: | 2013 |
| Předmět: |
Benzimidazole
medicine.drug_class Clinical Biochemistry Antiprotozoal Agents Pharmaceutical Science medicine.disease_cause Biochemistry Microbiology chemistry.chemical_compound Giardia intestinalis Entamoeba histolytica Drug Discovery medicine Trichomonas vaginalis Molecular Biology Hybrid biology Organic Chemistry Eukaryota Nitazoxanide biology.organism_classification Nitro Compounds Thiazoles chemistry Drug Design Antiprotozoal Molecular Medicine Protozoa Benzimidazoles Giardia lamblia medicine.drug |
| Zdroj: | Bioorganicmedicinal chemistry letters. 23(24) |
| ISSN: | 1464-3405 |
| Popis: | 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. |
| Databáze: | OpenAIRE |
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