Trypanocidal Activity Of 5,6-dihydropyran-2-ones Against Free Trypomastigotes Forms Of Trypanosoma Cruzi.

dc.creatorde Fátima, Angelo
dc.creatorMarquissolo, Cilene
dc.creatorde Albuquerque, Sergio
dc.creatorCarraro-Abrahão, Ana Amélia
dc.creatorPilli, Ronaldo Aloise
dc.date2006-Oct
dc.date2015-11-27T13:05:35Z
dc.date2015-11-27T13:05:35Z
dc.date.accessioned2018-03-29T01:03:03Z
dc.date.available2018-03-29T01:03:03Z
dc.identifierEuropean Journal Of Medicinal Chemistry. v. 41, n. 10, p. 1210-3, 2006-Oct.
dc.identifier0223-5234
dc.identifier10.1016/j.ejmech.2006.05.010
dc.identifierhttp://www.ncbi.nlm.nih.gov/pubmed/16815596
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/196832
dc.identifier16815596
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1297065
dc.descriptionSixteen 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).
dc.description41
dc.description1210-3
dc.languageeng
dc.relationEuropean Journal Of Medicinal Chemistry
dc.relationEur J Med Chem
dc.rightsfechado
dc.rights
dc.sourcePubMed
dc.subjectAnimals
dc.subjectDose-response Relationship, Drug
dc.subjectMolecular Structure
dc.subjectParasitic Sensitivity Tests
dc.subjectPyrones
dc.subjectStereoisomerism
dc.subjectStructure-activity Relationship
dc.subjectTrypanocidal Agents
dc.subjectTrypanosoma Cruzi
dc.titleTrypanocidal Activity Of 5,6-dihydropyran-2-ones Against Free Trypomastigotes Forms Of Trypanosoma Cruzi.
dc.typeArtículos de revistas


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