Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity

Abstract

Several aliphatic and aromatic lactones and two dimers were synthesized using the sequence: allylation - esterification - metathesis. These compounds were active in vitro against intracellular amastigotes of Leishmania panamensis. The structure-activity relationship showed the importance of the aliphatic side chain to enhance the biological activity and to obtain lower cytotoxicity. It was also observed that a decrease in the size of the lactone ring increases the selectivity index.

Keywords

• metathesis
• lactones
• antiparasite
• leishmania