Journal of the Brazilian Chemical Society
On-line version ISSN 1678-4790
ALVIM JR., Joel et al. Preparation and evaluation of a coumarin library towards the inhibitory activity of the enzyme gGAPDH from Trypanosoma cruzi. J. Braz. Chem. Soc. [online]. 2005, vol.16, n.4, pp. 763-773. ISSN 1678-4790. http://dx.doi.org/10.1590/S0103-50532005000500014.
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.
Keywords : Trypanosoma cruzi; coumarin library; chalepin; gGAPDH.