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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Format: | Article |
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MDPI AG
2009-07-01
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Series: | Molecules |
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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. |
first_indexed | 2024-12-11T00:37:02Z |
format | Article |
id | doaj.art-8d28ffbbcfa34d11944356eada6e1bc9 |
institution | Directory Open Access Journal |
issn | 1420-3049 |
language | English |
last_indexed | 2024-12-11T00:37:02Z |
publishDate | 2009-07-01 |
publisher | MDPI AG |
record_format | Article |
series | Molecules |
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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