Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/196832
Type: Artigo de periódico
Title: Trypanocidal Activity Of 5,6-dihydropyran-2-ones Against Free Trypomastigotes Forms Of Trypanosoma Cruzi.
Author: de Fátima, Angelo
Marquissolo, Cilene
de Albuquerque, Sergio
Carraro-Abrahão, Ana Amélia
Pilli, Ronaldo Aloise
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).
Subject: Animals
Dose-response Relationship, Drug
Molecular Structure
Parasitic Sensitivity Tests
Pyrones
Stereoisomerism
Structure-activity Relationship
Trypanocidal Agents
Trypanosoma Cruzi
Rights: fechado
Identifier DOI: 10.1016/j.ejmech.2006.05.010
Address: http://www.ncbi.nlm.nih.gov/pubmed/16815596
Date Issue: 2006
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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