Design, Synthesis And Biological Evaluation Of Hybrid Bioisoster Derivatives Of N-acylhydrazone And Furoxan Groups With Potential And Selective Anti-trypanosoma Cruzi Activity.

dc.creatorMassarico Serafim, Ricardo Augusto
dc.creatorGonçalves, José Eduardo
dc.creatorde Souza, Felipe Pereira
dc.creatorde Melo Loureiro, Ana Paula
dc.creatorStorpirtis, Silvia
dc.creatorKrogh, Renata
dc.creatorAndricopulo, Adriano Defini
dc.creatorDias, Luiz Carlos
dc.creatorFerreira, Elizabeth Igne
dc.date2014-Jul
dc.date2015-11-27T13:42:44Z
dc.date2015-11-27T13:42:44Z
dc.date.accessioned2018-03-29T01:21:04Z
dc.date.available2018-03-29T01:21:04Z
dc.identifierEuropean Journal Of Medicinal Chemistry. v. 82, p. 418-25, 2014-Jul.
dc.identifier1768-3254
dc.identifier10.1016/j.ejmech.2014.05.077
dc.identifierhttp://www.ncbi.nlm.nih.gov/pubmed/24929292
dc.identifierhttp://repositorio.unicamp.br/jspui/handle/REPOSIP/201479
dc.identifier24929292
dc.identifier.urihttp://repositorioslatinoamericanos.uchile.cl/handle/2250/1301712
dc.descriptionHybrid bioisoster derivatives from N-acylhydrazones and furoxan groups were designed with the objective of obtaining at least a dual mechanism of action: cruzain inhibition and nitric oxide (NO) releasing activity. Fifteen designed compounds were synthesized varying the substitution in N-acylhydrazone and in furoxan group as well. They had its anti-Trypanosoma cruzi activity in amastigotes forms, NO releasing potential and inhibitory cruzain activity evaluated. The two most active compounds (6, 14) both in the parasite amastigotes and in the enzyme contain the nitro group in para position of the aromatic ring. The permeability screening in Caco-2 cell and cytotoxicity assay in human cells were performed for those most active compounds and both showed to be less cytotoxic than the reference drug, benznidazole. Compound 6 was the most promising, since besides activity it showed good permeability and selectivity index, higher than the reference drug. Thereby the compound 6 was considered as a possible candidate for additional studies.
dc.description82
dc.description418-25
dc.languageeng
dc.relationEuropean Journal Of Medicinal Chemistry
dc.relationEur J Med Chem
dc.rightsfechado
dc.rightsCopyright © 2014 Elsevier Masson SAS. All rights reserved.
dc.sourcePubMed
dc.subjectAnti-trypanosoma Cruzi Compounds
dc.subjectBioisosters
dc.subjectFuroxan Derivatives
dc.subjectMolecular Hybrids
dc.subjectN-acylhydrazone Derivatives
dc.subjectNitric Oxide Donor Groups
dc.titleDesign, Synthesis And Biological Evaluation Of Hybrid Bioisoster Derivatives Of N-acylhydrazone And Furoxan Groups With Potential And Selective Anti-trypanosoma Cruzi Activity.
dc.typeArtículos de revistas


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