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. ©2005 Sociedade Brasileira de Química.
CITATION STYLE
Alvim, J., Dias, R. L. A., Castilho, M. S., Oliva, G., & Corrêa, A. G. (2005). Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi. Journal of the Brazilian Chemical Society, 16(4), 763–773. https://doi.org/10.1590/s0103-50532005000500014
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