Please use this identifier to cite or link to this item: http://repositorio.unicamp.br/jspui/handle/REPOSIP/201479
Type: Artigo de periódico
Title: Design, Synthesis And Biological Evaluation Of Hybrid Bioisoster Derivatives Of N-acylhydrazone And Furoxan Groups With Potential And Selective Anti-trypanosoma Cruzi Activity.
Author: Massarico Serafim, Ricardo Augusto
Gonçalves, José Eduardo
de Souza, Felipe Pereira
de Melo Loureiro, Ana Paula
Storpirtis, Silvia
Krogh, Renata
Andricopulo, Adriano Defini
Dias, Luiz Carlos
Ferreira, Elizabeth Igne
Abstract: Hybrid 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.
Subject: Anti-trypanosoma Cruzi Compounds
Bioisosters
Furoxan Derivatives
Molecular Hybrids
N-acylhydrazone Derivatives
Nitric Oxide Donor Groups
Rights: fechado
Identifier DOI: 10.1016/j.ejmech.2014.05.077
Address: http://www.ncbi.nlm.nih.gov/pubmed/24929292
Date Issue: 2014
Appears in Collections:Artigos e Materiais de Revistas Científicas - Unicamp

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