RESUMO
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 IC50 <12.5 µM (estimated 0.8 µM), lower than Benznidazole (IC50 = 9.8 µM), used as control. The esterification of acid diterpenes showed to be an interesting way in the search for anti-trypanosomal agents.
Assuntos
Diterpenos do Tipo Caurano , Diterpenos , Trypanosoma cruzi , Abietanos/farmacologia , Diterpenos do Tipo Caurano/farmacologiaRESUMO
In this paper, a complete 1 H and 13 C NMR data assignment of ent-polyalthic acid, a biologically active labdane-type diterpene, is presented. The assignments were carried on the basis of spectroscopic data from 1 H NMR, 13 C{1 H} NMR, gCOSY, gHMQC, and gHMBC experiments. Furthermore, a software-assisted methodology, using FOMSC3_rm_NB and NMR_MultSim programs, supported the detailed and unequivocal assignment of 1 H and 13 C signals, allowing all hydrogen coupling constants to be determined and thus clarifying all hydrogen signal multiplicities.
Assuntos
Diterpenos , Prótons , Isótopos de Carbono/química , Diterpenos/química , Espectroscopia de Ressonância Magnética/métodosRESUMO
A complete 1 H and 13 C NMR analysis for a group of four sesquiterpene lactones isolated from Eremanthus elaeagnus (Asteraceae) is described in this work. 1 H NMR, 13 C {1 H} NMR, gCOSY, gHMQC, and gHMBC experiments were performed to provide sufficient structural information to allow an unequivocal assignment. All hydrogen coupling constants were measured, clarifying all hydrogen signal multiplicities.
