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Novel triazine dimers with potent antitrypanosomal activity
Muthusamy Venkatraj1, Irene G Salado1, Jan Heeres1
1Laboratory of Medicinal Chemistry, University of Antwerp, Universiteitsplein 1, B-2610 Antwerp, Belgium.
European Journal of Medicinal Chemistry
|December 4, 2017
Summary
Researchers discovered novel triazine dimers with potent activity against Human African Trypanosomiasis (sleeping sickness). This finding offers hope for new treatments for this fatal neglected tropical disease.
Area of Science:
- Medicinal Chemistry
- Parasitology
- Drug Discovery
Background:
- Human African Trypanosomiasis (HAT), or sleeping sickness, is a fatal parasitic disease transmitted by tsetse flies, predominantly affecting impoverished rural African populations.
- Current treatments for HAT are limited, necessitating the development of safe and effective therapeutic options.
Purpose of the Study:
- To investigate the antitrypanosomal activity of triazine dimers.
- To optimize lead compounds for improved efficacy against HAT.
Main Methods:
- Phenotypic screening of triazine non-nucleoside HIV-1 reverse transcriptase inhibitors (monomers) identified initial antitrypanosomal compounds.
- Systematic optimization of identified triazine dimers led to the development of novel drug candidates.
Main Results:
- Optimization efforts yielded compound 38 (3,3'-(((ethane-1,2-diylbis(azanediyl))bis(4-(mesityloxy)-1,3,5-triazine-6,2-diyl))bis(azanediyl))dibenzonitrile).
- Compound 38 demonstrated highly potent in vitro and moderate in vivo antitrypanosomal activity.
Conclusions:
- Triazine dimers represent a promising class of compounds for HAT treatment.
- Compound 38 warrants further investigation as a potential therapeutic agent for sleeping sickness.
