SYNTHESIS OF 4-BENZYLSULFANYL AND 4-BENZYLSULFONYL CHALCONES. BIOLOGICAL EVALUATION AS ANTIMALARIAL AGENTS

Malaria management has been complicated in recent times, perhaps, by increasing the Plasmodium spp. resistance to the drugs of clinical use for its treatment. The study describes the synthesis of a new series of chalcones 7 - 40 and their antimalarial efficacy against a chloroquine-susceptible strain of Plasmodium berghei. Furthermore, we carried out hemindependent studies to unfold the mechanism of action of these synthesized hybrid molecules. Twenty compounds showed inhibitory activity on the formation of beta-hematin higher than 75%, compared to chloroquine. The compounds 9, 21, 33 and 37 showed enhanced antimalarial activity in vivo and may reduce malaria progression in this model through a mechanism related to the inhibition of hemozoin formation. Critical aspects of the structure-activity relationship (SAR) are also discussed to better understand the effect shown by these compounds.

Automated summary

The study successfully synthesized a new series of chalcones and evaluated their antimalarial efficacy. Some of the compounds showed high inhibitory activity and potentially slow down the progression of malaria through inhibition of hemozoin formation. The study also discussed critical aspects of the structure-activity relationship.