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|Type:||Artigo de periódico|
|Title:||Trypanocidal Activity Of 5,6-dihydropyran-2-ones Against free Trypomastigotes Forms Of trypanosoma cruzi|
|Author:||de Fatima A.|
de Albuquerque S.
|Abstract:||Sixteen 5,6-dihydro-2H-pyran-2-ones were evaluated in in vitro assay against trypomastigotes forms of Trypanosoma cruzi, the causative agent of Chagas' disease. A structure-activity relationship study (SAR) allowed us to establish the relevant structural features for the trypanocidal activity of goniothalamin analogues against T. cruzi. In fact, non-natural form of goniothalamin (ent-1) was threefold more potent than the natural one (1). In addition, we have identified analogues 9 and 10 (both displaying S configuration) as the highest potent compounds against T. cruzi with IC50 = 0.12 and 0.09 mM (IC50 value for crystal violet was 0.08 mM) whereas significantly lower toxicities were observed when these compounds were evaluated under LLC-MK2 lineage cells (1.38 and 4.89 mM, respectively). In addition, epoxides derivatives 12 and ent-12 were shown to be more potent than the corresponding stereoisomers 2 and ent-2 and non-natural argentilactone (ent-3, IC50 = 0.47 mM) was twofold more potent than natural argentilactone (3, IC50 = 0.94 mM). © 2006 Elsevier Masson SAS. All rights reserved.|
|Appears in Collections:||Unicamp - Artigos e Outros Documentos|
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