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

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 alip...

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Bibliographic Details
Main Authors: Fernando Echeverri, Wilson Cardona, Sara Robledo, Winston Quiñones, Marcela Castaño
Format: Article
Language:English
Published: MDPI AG 2009-07-01
Series:Molecules
Subjects:
Online Access:http://www.mdpi.com/1420-3049/14/7/2491/
Description
Summary: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.
ISSN:1420-3049