Introduction

The invention refers to a new class of compounds with a 5- (2-nitroethyl) -2,4,6-triaminopyrimidine structure used as antiparasitic agents, in particular against the parasites Trypanosoma brucei and Trypanosoma cruzie (Chagas disease), cause of the diseases African Human Trypanosomiasis (or sleeping sickness).

Technical features

The patented compounds were designed and developed as inhibitors of the parasitic enzyme Pteridine-reductase 1 (PTR1). PTR1 is a specific enzyme of this parasitic family and is absent in humans and provides, in these parasites, the need for tetrahydrofolic acid when dihydrofolate reductase is inhibited by traditional antifolate drugs, which are therefore ineffective in the treatment of these parasitic infections. PTR1 therefore represents an interesting target for the development of new potential therapeutic agents capable of counteracting these parasitic infections.
The technology achieves TRL=3

Possible Applications

• Therapy of “neglected” tropical diseases (NTD-Neglected Tropical Diseases) with protozoan etiology;
• They can be used against other protozoa;
• They can be developed for animal use.

Advantages

• Less toxicity to humans than the drugs in use;
• Capacity to overcome drug resistance;
• Easy to synthesize.