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dc.contributor.CRUESPUNIVERSIDADE DE ESTADUAL DE CAMPINASpt_BR
dc.typeArtigo de periódicopt_BR
dc.titleNew Antibacterial Agents: Hybrid Bioisoster Derivatives As Potential E. Coli Fabh Inhibitorspt_BR
unicamp.author.emailelizabeth.igne@gmail.compt_BR
unicamp.authorSegretti, M.C.F., Universidade Estadual de Campinas, Instituto de Química, Cidade Universitária ‘Zeferino Vaz’, Distrito de Barão Geraldo, 13083-970, CampinasSP, Brazilpt_BR
unicamp.author.externalSegretti, N.D., Universidade de São Paulo, Faculdade de Ciências Farmacêuticas, Departamento de Farmácia, Av. Prof. Lineu Prestes, 580SP, Brazilpt
unicamp.author.externalSerafim, R.A.M., Universidade de São Paulo, Faculdade de Ciências Farmacêuticas, Departamento de Farmácia, Av. Prof. Lineu Prestes, 580SP, Brazilpt
unicamp.author.externalMiyata, M., Universidade Estadual Paulista ‘Júlio de Mesquita Filho’, Faculdade de Ciências Farmacêuticas, Departamento de Ciências Biológicas, Rodovia Araraquara-Jaú km 1, Araraquara, SP, Brazilpt
unicamp.author.externalCoelho, F.R., Universidade de São Paulo, Instituto de Química, Departamento de Bioquímica, 748SP, Brazilpt
unicamp.author.externalAugusto, O., Universidade de São Paulo, Instituto de Química, Departamento de Bioquímica, 748SP, Brazilpt
unicamp.author.externalFerreira, E.I., Universidade de São Paulo, Faculdade de Ciências Farmacêuticas, Departamento de Farmácia, Av. Prof. Lineu Prestes, 580SP, Brazilpt
dc.description.abstractThe development of resistance to antibiotics by microorganisms is a major problem for the treatment of bacterial infections worldwide, and therefore, it is imperative to study new scaffolds that are potentially useful in the development of new antibiotics. In this regard, we propose the design, synthesis and biological evaluation of hybrid sulfonylhydrazone bioisosters/furoxans with potential antibacterial (Escherichia coli) activity. The most active compound of the series, (E)-3-methyl-4-((2-tosylhydrazono)methyl)-1,2,5-oxadiazole 2-oxide, with a MIC = 0.36 μM, was not cytotoxic when tested on Vero cells (IC50 >100 μM). To complement the in vitro screening, we also studied the interaction of the test compounds with β-ketoacyl acyl carrier protein synthase (FabH), the target for the parent compounds, and we observed three important hydrogen-bonding interactions with two important active site residues in the catalytic site of the enzyme, providing complementary evidence to support the target of the new hybrid molecules. © 2016 Elsevier Ltden
dc.relation.ispartofBioorganic and Medicinal Chemistry Letterspt_BR
dc.publisherElsevier Ltdpt_BR
dc.date.issued2016pt_BR
dc.identifier.citationBioorganic And Medicinal Chemistry Letters. Elsevier Ltd, v. 26, p. 3988 - 3993, 2016.pt_BR
dc.language.isoenpt_BR
dc.description.volume26pt_BR
dc.description.issuenumberpt_BR
dc.description.firstpage3988pt_BR
dc.description.lastpage3993pt_BR
dc.rightsfechadopt_BR
dc.sourceScopuspt_BR
dc.identifier.issn0960894Xpt_BR
dc.identifier.doi10.1016/j.bmcl.2016.06.089pt_BR
dc.identifier.urlhttps://www.scopus.com/inward/record.uri?eid=2-s2.0-84979539452&partnerID=40&md5=5a6d18290931c69be5ec39c8a0651733pt_BR
dc.date.available2016-12-06T17:43:06Z-
dc.date.accessioned2016-12-06T17:43:06Z-
dc.description.provenanceMade available in DSpace on 2016-12-06T17:43:06Z (GMT). No. of bitstreams: 1 2-s2.0-84979539452.pdf: 1473499 bytes, checksum: 14df53d818b756a1ebc9891a3af51844 (MD5) Previous issue date: 2016en
dc.identifier.urihttp://repositorio.unicamp.br/jspui/handle/REPOSIP/319260-
dc.identifier.idScopus2-s2.0-84979539452pt_BR
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