The in vitro antiplasmodial activity of some dihydrostilbenamides, phtalazinones, imidazo[2,1-a]isoindole and pyrimido[2,1-a]isoindole derivatives related to the natural dihydrostilbenoid isonotholaenic acid is reported. The evaluation was performed on cultures of F32 strain of Plasmodium falciparum and potent representative compounds were also evaluated in the ferriprotoporphyrin IX biomineralization inhibition test (FBIT). Compounds having the imidazo[2,1-a]isoindole skeleton were the most active and one compound of this group resulted to be as potent as chloroquine, but acting through a mechanism different that of the inhibition of heme biomineralization.
Bibliographical noteFunding Information:
M.G.A. thanks AECI (Spain) for a fellowship. M.I.Y. thanks the University of Tucuman (Argentina) for the support. Financial support of the chemical part came from Spanish DGICYT (SAF 98/0103). Biological evaluations were supported by the Institut de Recherche pour le Développement (IRD-France) and the OAS (OEA-Regional Flora). This collaborative work has been performed under the auspices of the Ibero-American Program of Science and Technology for Development (CYTED), Sub-Program X.