In vitro anti-trypanosomal potential of kaurane and pimarane semi-synthetic derivatives.

As part of the search for anti-trypanosomal agents, this work presents the production of sixteen derivatives. All of them were obtained from two natural diterpenes, one with kaurane skeleton ( ent -kaurenoic acid) and other with a pimarane skeleton ( ent -pimaradienoic acid). Then, the eighteen compounds were assayed against epimastigote form of Trypanosoma cruzi , with the derivatives showing increase of activity in relation to their precursors. Moreover, the most active derivative presented an IC ₅₀ <12.5 µM (estimated 0.8 µM), lower than Benznidazole (IC ₅₀ = 9.8 µM), used as control. The esterification of acid diterpenes showed to be an interesting way in the search for anti-trypanosomal agents.