Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/103469
Type: Artigo de periódico
Title: Trypanocidal Activity Of 5,6-dihydropyran-2-ones Against free Trypomastigotes Forms Of trypanosoma cruzi
Author: de Fatima A.
Marquissolo C.
de Albuquerque S.
Carraro-Abrahao A.A.
Pilli R.A.
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.
Editor: 
Rights: fechado
Identifier DOI: 10.1016/j.ejmech.2006.05.010
Address: http://www.scopus.com/inward/record.url?eid=2-s2.0-33749643183&partnerID=40&md5=1112cd03fbf4a9d228cb9ee53b3dadbe
Date Issue: 2006
Appears in Collections:Unicamp - Artigos e Outros Documentos

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