As a part of our actual antiprotozoal lead optimization project, five new nicotinamide derivatives were synthesized and in vitro tested against Plasmodium berghei, Trypanosoma cruzi, Giardia intestinalis and Leismania mexicana. Although all compounds showed moderate antiparasitic activity and low cytotoxicity, three of them presented interesting antiplasmodial activity. These compounds would interact with SIR2, a protein identified in Plasmodium berghei as a novel target for the design of antiprotozoal agents. The synthesis, spectroscopic data and biological tests will be presented.

Synthesis and antiprotozoal activity of nicotinamide derivatives

244th National Meeting (2012)

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