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Control and treatment of onchocerciasis, a devastating tropical filarial disease caused by Onchocerca volvulus, rely solely on the community directed treatment with ivermectin. However, ivermectin is only microfilaricidal with evidence of resistance of the parasite among other limitations, which necessitate the search for new efficacious and safe filaricides. Ten synthetic thienylazoryl dyes were screened in vitro against adult and microfilariae worm stages of Onchocerca ochengi based on worm motility and MTT formazan assay. Cytotoxicity of active compounds was assessed on monkey kidney epithelial cells (LLC-MK2) using the MTT formazan assay. Seven (7) compounds showed both macrofilaricidal activity against adult male worms and microfilaricidal activity among which three 4a, 4c and 4e recorded the highest activity (IC50 = 4.2 to 8.8μM) against adult male worms, comparable to some standard anthelmintics. Five compounds showed rapid activity against microfilariae with 100% inhibition after 24-h incubation. The active compounds were nontoxic on monkey kidney cells (CC50> 4μg/mL), but their selectivity index values were relatively low (≤ 3). The thienylazoaryls with both macrofilaricidal and microfilaricidal activities may yield molecules which could be used for eradication of onchocerciasis following further medicinal chemistry modification of their structures to enhance their selectivity.

Citation

Joseph Tsemeugne, Lahngong M Shinyuy, Sorel K D Djeukoua, Emmanuel F Sopbue, Moses N Ngemenya. Evaluation of macrofilaricidal and microfilaricidal activities against Onchocerca ochengi and cytotoxicity of some synthesized azo compounds containing thiophene backbone. Parasitology research. 2021 Jun;120(6):2087-2094

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PMID: 33864105

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