AI Article Synopsis
- Human African trypanosomiasis (HAT), or sleeping sickness, is a deadly disease caused by parasites transmitted through the bite of tsetse flies, primarily affecting impoverished communities in rural Africa.
- Currently, there are limited safe and effective treatments for HAT, but researchers have identified promising antitrypanosomal compounds through screening triazine-based HIV-1 inhibitors.
- Further optimization of triazine dimers led to the development of a specific compound (compound 38) that demonstrated strong in vitro efficacy and moderate effectiveness in vivo against the disease.
Article Abstract
Human African trypanosomiasis (HAT), also known as sleeping sickness is a parasitic disease transmitted by the bite of the 'Glossina' insect, commonly known as the tsetse fly. This disease affects mostly poor populations living in remote rural areas of Africa. Untreated, it is usually fatal. Currently, safe and effective treatments against this disease are lacking. Phenotypic screening of triazine non-nucleoside HIV-1 reverse transcriptase inhibitors (monomers) resulted in potent and selective antitrypanosomal compounds. This serendipitous discovery and the presence of dimers in many compounds active against these neglected tropical diseases prompted us to investigate antitrypanosomal activity of triazine dimers. Optimization of the triazine dimers resulted in 3,3'-(((ethane-1,2-diylbis(azanediyl))bis(4-(mesityloxy)-1,3,5-triazine-6,2-diyl))bis(azanediyl))dibenzonitrile (compound 38), a compound with very potent in vitro and moderate in vivo antitrypanosomal activity.
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| http://dx.doi.org/10.1016/j.ejmech.2017.11.075 | DOI Listing |
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