Leishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivatives

Página do item simplificado
dc.contributor.authorDutra, Luiz Antonio [UNESP]
dc.contributor.authorAlmeida, Leticia de [UNESP]
dc.contributor.authorPassalacqua, Thais G. [UNESP]
dc.contributor.authorReis, Juliana Santana [UNESP]
dc.contributor.authorTorres, Fabio A. E. [UNESP]
dc.contributor.authorMartinez, Isabel [UNESP]
dc.contributor.authorPeccinini, Rosangela Goncalves [UNESP]
dc.contributor.authorChin, Chung Man [UNESP]
dc.contributor.authorChegaev, Konstantin
dc.contributor.authorGuglielmo, Stefano
dc.contributor.authorFruttero, Roberta
dc.contributor.authorGraminha, Márcia Aparecida Silva [UNESP]
dc.contributor.authorSantos, Jean Leandro dos [UNESP]
dc.contributor.institutionUniversidade Estadual Paulista (Unesp)
dc.contributor.institutionUniv Turin
dc.date.accessioned2014-12-03T13:09:13Z
dc.date.available2014-12-03T13:09:13Z
dc.date.issued2014-08-01
dc.description.abstractA novel series of furoxan (1,2,5-oxadiazole 2-oxide) (compounds 3, 4a and -b, 13a and -b, and 14a to -f) and benzofuroxan (benzo[c][1,2,5] oxadiazole 1-oxide) (compounds 7 and 8a to -c) derivatives were synthesized, characterized, and evaluated for in vitro activity against promastigote and intracellular amastigote forms of Leishmania amazonensis. The furoxan derivatives exhibited the ability to generate nitric oxide at different levels (7.8% to 27.4%). The benzofuroxan derivative 8a was able to increase nitrite production in medium supernatant from murine macrophages infected with L. amazonensis at 0.75 mM after 48 h. Furoxan and benzofuroxan derivatives showed remarkable leishmanicidal activity against both promastigote and intracellular amastigote forms. Compounds 8a, 14a and -b, and 14d exerted selective leishmanicidal activities superior to those of amphotericin B and pentamidine. In vitro studies at pH 5.4 reveal that compound 8a is stable until 8 h and that compound 14a behaves as a prodrug, releasing the active aldehyde 13a. These compounds have emerged as promising novel drug candidates for the treatment of leishmaniasis.en
dc.description.affiliationUniv Estadual Paulista UNESP, Fac Ciencias Farmaceut, Araraquara, SP, Brazil
dc.description.affiliationUniv Turin, Dipartimento Sci & Tecnol Farmaco, Turin, Italy
dc.description.affiliationUnespUniv Estadual Paulista UNESP, Fac Ciencias Farmaceut, Araraquara, SP, Brazil
dc.description.sponsorshipFundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)
dc.description.sponsorshipCoordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES)
dc.description.sponsorshipPrograma de Estagio no Exterior (PROPG-UNESP)
dc.description.sponsorshipIdFAPESP: 12/50359-2
dc.description.sponsorshipIdFAPESP: 11/15520-4
dc.description.sponsorshipIdCAPES: 455903/2012-3
dc.description.sponsorshipIdCAPES: 310026/2011-3
dc.format.extent4837-4847
dc.identifierhttp://dx.doi.org/10.1128/AAC.00052-14
dc.identifier.citationAntimicrobial Agents And Chemotherapy. Washington: Amer Soc Microbiology, v. 58, n. 8, p. 4837-4847, 2014.
dc.identifier.doi10.1128/AAC.00052-14
dc.identifier.fileWOS000339259200069.pdf
dc.identifier.issn0066-4804
dc.identifier.lattes1066743423929093
dc.identifier.lattes9734333607975413
dc.identifier.orcid0000-0003-4141-0455
dc.identifier.urihttp://hdl.handle.net/11449/112081
dc.identifier.wosWOS:000339259200069
dc.language.isoeng
dc.publisherAmer Soc Microbiology
dc.relation.ispartofAntimicrobial Agents and Chemotherapy
dc.relation.ispartofjcr4.255
dc.relation.ispartofsjr2,291
dc.rights.accessRightsAcesso restrito
dc.sourceWeb of Science
dc.titleLeishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivativesen
dc.typeArtigo
dcterms.rightsHolderAmer Soc Microbiology
unesp.author.lattes1066743423929093
unesp.author.lattes9734333607975413[8]
unesp.author.orcid0000-0001-7280-3775[12]
unesp.author.orcid0000-0003-4141-0455[8]
unesp.campusUniversidade Estadual Paulista (Unesp), Faculdade de Ciências Farmacêuticas, Araraquarapt

Arquivos

Pacote Original
Agora exibindo 1 - 1 de 1
Imagem de Miniatura
Nome:
WOS000339259200069.pdf
Tamanho:
1.29 MB
Formato:
Adobe Portable Document Format
Baixar

Coleções

Artigos - Princípios Ativos Naturais e Toxicologia - FCFAR
Artigos - Fármacos e Medicamentos - FCFAR