Synthesis of chlorovinyl sulfones as structural analogs of chalcones and their antiplasmodial activities

The synthesis of novel chlorovinyl sulfone-like chalcone derivatives and their antimalarial activity against cultured Plasmodium falciparum parasites, hemozoin formation, hemoglobin hydrolysis and murine malaria model are described. Compounds were prepared via Claisen–Schmidt condensation from available chloromethylphenyl sulfones with substituted aldehydes. Antiplasmodial IC50 activity of these compounds ranged between 0.025 and 10 μM, those that blocked P. falciparum development at low micro molar concentrations were tested in a murine Plasmodium berghei model, and these compounds delayed the progression of malaria but did not eradicate infections. Much effort and attention are needed for discovery and development of new and less toxic antimalarial drugs.

Graphical abstractThe synthesis and antimalarial activity in vitro and in vivo of a new series of chlorovinyl sulfone analogs of chalcones are described.Figure optionsDownload full-size imageDownload as PowerPoint slide