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 t...

Full description

Saved in:
Bibliographic Details
Published in:Journal of the Brazilian Chemical Society Vol. 16; no. 4; pp. 763 - 773
Main Authors: Alvim Jr, Joel, Dias, Ricardo L. A., Castilho, Marcelo S., Oliva, Glaucius, Corrêa, Arlene G.
Format: Journal Article
Language:English
Published: Sociedade Brasileira de Química 01-08-2005
Subjects:
CHEMISTRY, MULTIDISCIPLINARY
gGAPDH
coumarin library
chalepin
Trypanosoma cruzi
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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.
ISSN:0103-5053
1678-4790
DOI:10.1590/S0103-50532005000500014