Ricerc@Sapienza

We have designed and synthesized a series of new imidazole-based compounds structurally related to an antiprotozoal agent with nanomolar activity which we identified recently. The new analogs possess micromolar activities against T. b. rhodesiense and L. donovani and nanomolar potency against P. falciparum. Most of the analogs displayed the IC50 within the low nanomolar range against T. cruzi, with very high selectivity towards the parasite. Discussion of structure-activity relationships and in vitro biological data for the new compounds are provided against a number of different protozoa.

The rationale inspiring the discovery of lead compounds for the treatment of humanparasitic protozoan diseases from natural sources is the well-established use of medicinal plantsin various systems of traditional medicine. On this basis, we decided to select an overlookedmedicinal plant growing in central Italy,Marrubium incanumDesr.(Lamiaceae), which hasbeen used as a traditional remedy against protozoan diseases, and to investigate its potentialagainst Human African trypanosomiasis (HAT).