Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi

Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi

Chagas' disease, caused by Trypanosoma cruzi, is endemic in 15 countries in Latin America. In this work a library of 38 coumarins was prepared in solution phase and evaluated against T. cruzi glycolytic enzyme glyceraldehyde-3-phosphate-dehydrogenase (gGAPDH). The synthetic route was based on the Knoevenagel condensation of different 2-hydroxybenzaldehydes with Meldrum's acid or diethyl malonate, followed by O-alkylation and/or transesterification reactions. Among the prepared coumarins, the best values obtained to inhibit 50% of the enzymatic activity range from 80 to 130 µM.

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Main Authors: Alvim Jr.,Joel, Dias,Ricardo L. A., Castilho,Marcelo S., Oliva,Glaucius, Corrêa,Arlene G.
Format: Digital revista
Language:English
Published: Sociedade Brasileira de Química 2005
Online Access:http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532005000500014
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spelling oai:scielo:S0103-505320050005000142005-08-25Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruziAlvim Jr.,JoelDias,Ricardo L. A.Castilho,Marcelo S.Oliva,GlauciusCorrêa,Arlene G. Trypanosoma cruzi coumarin library chalepin gGAPDH Chagas' disease, caused by Trypanosoma cruzi, is endemic in 15 countries in Latin America. In this work a library of 38 coumarins was prepared in solution phase and evaluated against T. cruzi glycolytic enzyme glyceraldehyde-3-phosphate-dehydrogenase (gGAPDH). The synthetic route was based on the Knoevenagel condensation of different 2-hydroxybenzaldehydes with Meldrum's acid or diethyl malonate, followed by O-alkylation and/or transesterification reactions. Among the prepared coumarins, the best values obtained to inhibit 50% of the enzymatic activity range from 80 to 130 µM.info:eu-repo/semantics/openAccessSociedade Brasileira de QuímicaJournal of the Brazilian Chemical Society v.16 n.4 20052005-08-01info:eu-repo/semantics/articletext/htmlhttp://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532005000500014en10.1590/S0103-50532005000500014
institution SCIELO
collection OJS
country Brasil
countrycode BR
component Revista
access En linea
databasecode rev-scielo-br
tag revista
region America del Sur
libraryname SciELO
language English
format Digital
author Alvim Jr.,Joel
Dias,Ricardo L. A.
Castilho,Marcelo S.
Oliva,Glaucius
Corrêa,Arlene G.
spellingShingle Alvim Jr.,Joel
Dias,Ricardo L. A.
Castilho,Marcelo S.
Oliva,Glaucius
Corrêa,Arlene G.
Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi
author_facet Alvim Jr.,Joel
Dias,Ricardo L. A.
Castilho,Marcelo S.
Oliva,Glaucius
Corrêa,Arlene G.
author_sort Alvim Jr.,Joel
title Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi
title_short Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi
title_full Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi
title_fullStr Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi
title_full_unstemmed Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi
title_sort preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme ggapdh from trypanosoma cruzi
description Chagas' disease, caused by Trypanosoma cruzi, is endemic in 15 countries in Latin America. In this work a library of 38 coumarins was prepared in solution phase and evaluated against T. cruzi glycolytic enzyme glyceraldehyde-3-phosphate-dehydrogenase (gGAPDH). The synthetic route was based on the Knoevenagel condensation of different 2-hydroxybenzaldehydes with Meldrum's acid or diethyl malonate, followed by O-alkylation and/or transesterification reactions. Among the prepared coumarins, the best values obtained to inhibit 50% of the enzymatic activity range from 80 to 130 µM.
publisher Sociedade Brasileira de Química
publishDate 2005
url http://old.scielo.br/scielo.php?script=sci_arttext&pid=S0103-50532005000500014
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