MIPS researchers develop potential new cures for Chagas Disease
A new class of trypanosomacides has been synthesised by MIPS research teams headed by Professor Jonathan Baell and Dr Raphael Rahmani.
The research, which features on the cover of the Journal of Medicinal Chemistry, outlines a new generation of compounds that target the parasites Trypanosoma brucei and T. cruzi. These parasitic agents are responsible for significant human suffering in the form of Human African Trypanosomiasis (HAT) and Chagas disease. Drugs currently available to treat these neglected diseases have high patient noncompliance due to their toxic side-effects.
The study identifies a new library of compounds belonging to the substituted thiazole class, with one compound clearing all signs of T. cruzi infection in mice when co-administered with a CYP (metabolising enzyme) inhibitor. CYP inhibition decreases the rate in which the trypanosomacide is metabolised, a common hurdle observed in the thiazole class of compounds. The group hopes to further this study by optimising the compounds to be more metabolically stable. The paper, ‘Hit-to-Lead Optimization of a Novel Class of Potent, Broad-Spectrum Trypanosomacides, is published in J.Med Chem (DOI: 10.1021/acs.jmedchem.6b00442).
The article can be accessed here.