Introduction

The invention refers to a new class of compounds usable for the treatment of Leishmaniosis, sleeping sickness and Chagas disease, having the chromen-4-one ring linked to different heteroaromatic rings.

These antiparasitic agents, active against infections by Leishmania spp, Trypanosoma brucei and Trypanosoma cruzi, overcome resistance response showed by current drugs

Technical features

The novel antiparasitic compounds are active against drug resistance parasites; H80 compound shows, in experiments presented in the patent, the antiparasitic activity still evident in strains of drug resistance Leishmania specie.
In particular tests are about field isolates of L. donovani from Nepal, BPK091 and BPK190, inherently sensitive and resistant to antimony treatment, respectively , but same results have been observed in different resistant strains from the field. Additionally RNAseq experiments did not show the generation of overexpressed proteins linked to H80 activity.
In vivo experiments showed low toxicity and interesting PK profile; as per these experiments, the technology achieves TRL=3

Possible Applications

• Starting point for the optimization towards a lead;
• Broad spectrum antiparasitic lead against Leishmania spp, Trypanosoma brucei and Trypanosoma cruzi;
• Drug for antiparasitic trypanosomatidic infections.

Advantages

• Parasite growth inhibition, even with strains resistant to the known antiparasitic drugs;
• Optimal starting lead;
• Non toxic compound;
• Capacity to overcome drug resistance;
• Easy to synthesize.