Fenarimol, a plant fungicide, was found to be a potent inhibitor of Trypanosoma cruzi, the parasite which causes Chagas disease, and was chosen as a starting point for lead optimisation to improve its activity. A large number of very active and selective inhibitors of T.cruzi were easily synthesized in large quantities and a “scaffold-hopping” exercise created new opportunities, leading to the discovery of an extensive family of novel inhibitors with high oral bioavailability, long half-life and high efficacy.

We have previously released data pertaining to 751 compounds. This second release includes data on a further 84 compounds from the two more advanced series of fenarimols which include the preclinical candidates EPL-BS0967 and EPL-BS1246, both of which are T.cruzi CYP51 inhibitors.

More information