期刊
JOURNAL OF THE BRAZILIAN CHEMICAL SOCIETY
卷 16, 期 4, 页码 763-773出版社
SOC BRASILEIRA QUIMICA
DOI: 10.1590/S0103-50532005000500014
关键词
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 mu M.
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