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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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/
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author Fernando Echeverri
Wilson Cardona
Sara Robledo
Winston Quiñones
Marcela Castaño
author_facet Fernando Echeverri
Wilson Cardona
Sara Robledo
Winston Quiñones
Marcela Castaño
author_sort Fernando Echeverri
collection DOAJ
description 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.
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spelling doaj.art-8d28ffbbcfa34d11944356eada6e1bc92022-12-22T01:27:07ZengMDPI AGMolecules1420-30492009-07-011472491250010.3390/molecules14072491Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-ActivityFernando EcheverriWilson CardonaSara RobledoWinston QuiñonesMarcela CastañoSeveral 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.http://www.mdpi.com/1420-3049/14/7/2491/metathesislactonesantiparasiteleishmania
spellingShingle Fernando Echeverri
Wilson Cardona
Sara Robledo
Winston Quiñones
Marcela Castaño
Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
Molecules
metathesis
lactones
antiparasite
leishmania
title Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
title_full Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
title_fullStr Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
title_full_unstemmed Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
title_short Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
title_sort leishmanicidal activity of aliphatic and aromatic lactones correlation structure activity
topic metathesis
lactones
antiparasite
leishmania
url http://www.mdpi.com/1420-3049/14/7/2491/
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