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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Detalles Bibliográficos
Autores principales: Castaño, Marcela, Cardona, Wilson, Quiñones, Winston, Robledo, Sara, Echeverri, Fernando
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Molecular Diversity Preservation International 2009
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6255270/
https://www.ncbi.nlm.nih.gov/pubmed/19633618
http://dx.doi.org/10.3390/molecules14072491
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author Castaño, Marcela
Cardona, Wilson
Quiñones, Winston
Robledo, Sara
Echeverri, Fernando
author_facet Castaño, Marcela
Cardona, Wilson
Quiñones, Winston
Robledo, Sara
Echeverri, Fernando
author_sort Castaño, Marcela
collection PubMed
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 pubmed-62552702018-11-30 Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity Castaño, Marcela Cardona, Wilson Quiñones, Winston Robledo, Sara Echeverri, Fernando Molecules Article 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. Molecular Diversity Preservation International 2009-07-10 /pmc/articles/PMC6255270/ /pubmed/19633618 http://dx.doi.org/10.3390/molecules14072491 Text en © 2009 by the authors; licensee Molecular Diversity Preservation International, Basel, Switzerland. This article is an open access article distributed under the terms and conditions of the Creative Commons Attribution license (http://creativecommons.org/licenses/by/3.0/).
spellingShingle Article
Castaño, Marcela
Cardona, Wilson
Quiñones, Winston
Robledo, Sara
Echeverri, Fernando
Leishmanicidal Activity of Aliphatic and Aromatic Lactones: Correlation Structure-Activity
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 Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC6255270/
https://www.ncbi.nlm.nih.gov/pubmed/19633618
http://dx.doi.org/10.3390/molecules14072491
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