Aurones A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents英文文献资料.docVIP
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Aurones A Promising Heterocyclic Scaffold for the Development of Potent Antileishmanial Agents英文文献资料
HindawiPublishingCorporation
InternationalJournalofMedicinalChemistry
Volume2012,ArticleID196921,8pages
doi:10.1155/2012/196921
ResearchArticle
Aurones:APromisingHeterocyclicScaffoldfortheDevelopment
ofPotentAntileishmanialAgents
MarinaRoussaki, So?aCostaLima, Anna-MariaKypreou, PanagiotisKefalas,
1 2 1 3
AnabelaCordeirodaSilva,2,4andAnastasiaDetsi1
1
2
3
4
LaboratoryofOrganicChemistry,SchoolofChemicalEngineering,NationalTechnicalUniversityofAthens,
HeroonPolytechniou9,ZografouCampus,15780Athens,Greece
ParasiteDiseaseGroup,IBMC-InstituteforMolecularandCellBiology,UniversityofPorto,RuadoCampoAlegre,
823,4150-180Porto,Portugal
DepartmentofFoodQualityandChemistryofNaturalProducts,MediterraneanAgronomicInstituteofChania,
InternationalCentreforAdvancedMediterraneanAgronomicStudies,73100Chania,Crete,Greece
DepartmentofBiologicalSciences,FacultyofPharmacy,UniversityofPorto,RuadeJorgeViterboFerreiera,
228,4050-313Porto,Portugal
CorrespondenceshouldbeaddressedtoAnastasiaDetsi,adetsi@chemeng.ntua.gr
Received27May2012;Accepted31July2012
AcademicEditor:O.Bruno
Copyright?2012MarinaRoussakietal. This is an open access article distributed under the Creative Commons Attribution
License,whichpermitsunrestricteduse,distribution,andreproductioninanymedium,providedtheoriginalworkisproperly
cited.
A series of (Z)-2-benzylidenebenzofuran-3-(2H)-ones (aurones) bearing a variety of substituents on rings A and B were
synthesizedandevaluatedfortheirantiparasiticactivityagainsttheintracellularamastigoteformofLeishmaniainfantumandtheir
cytotoxicityagainsthumanTHP1-di?erentiatedmacrophages.Ingeneral,auronesbearingnosubstituentsonringA(compounds
4a–4f)exhibithighertoxicitythanauroneswith4,6-dimethoxysubstitution(compounds4g–4l).Amongthelatter,twoaurones
possessinga2-methoxyora2-methylgroup(compounds4iand4j)exhibitpotentantileishmanialactivity(IC50=1.3± 0.1μM
andIC50=1.6±0.2μM,resp.),comparabletotheactivityofthereferenced
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