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http://acervodigital.unesp.br/handle/11449/112081
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DC Field | Value | Language |
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dc.contributor.author | Dutra, Luiz Antonio | - |
dc.contributor.author | Almeida, Leticia de | - |
dc.contributor.author | Passalacqua, Thais G. | - |
dc.contributor.author | Reis, Juliana Santana | - |
dc.contributor.author | Torres, Fabio A. E. | - |
dc.contributor.author | Martinez, Isabel | - |
dc.contributor.author | Peccinini, Rosangela Goncalves | - |
dc.contributor.author | Chin, Chung Man | - |
dc.contributor.author | Chegaev, Konstantin | - |
dc.contributor.author | Guglielmo, Stefano | - |
dc.contributor.author | Fruttero, Roberta | - |
dc.contributor.author | Graminha, Márcia Aparecida Silva | - |
dc.contributor.author | Santos, Jean Leandro dos | - |
dc.date.accessioned | 2014-12-03T13:09:13Z | - |
dc.date.accessioned | 2016-10-25T20:10:23Z | - |
dc.date.available | 2014-12-03T13:09:13Z | - |
dc.date.available | 2016-10-25T20:10:23Z | - |
dc.date.issued | 2014-08-01 | - |
dc.identifier | http://dx.doi.org/10.1128/AAC.00052-14 | - |
dc.identifier.citation | Antimicrobial Agents And Chemotherapy. Washington: Amer Soc Microbiology, v. 58, n. 8, p. 4837-4847, 2014. | - |
dc.identifier.issn | 0066-4804 | - |
dc.identifier.uri | http://hdl.handle.net/11449/112081 | - |
dc.identifier.uri | http://acervodigital.unesp.br/handle/11449/112081 | - |
dc.description.abstract | A 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.sponsorship | Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP) | - |
dc.description.sponsorship | Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES) | - |
dc.description.sponsorship | Programa de Estagio no Exterior (PROPG-UNESP) | - |
dc.format.extent | 4837-4847 | - |
dc.language.iso | eng | - |
dc.publisher | Amer Soc Microbiology | - |
dc.source | Web of Science | - |
dc.title | Leishmanicidal Activities of Novel Synthetic Furoxan and Benzofuroxan Derivatives | en |
dc.type | outro | - |
dc.contributor.institution | Universidade Estadual Paulista (UNESP) | - |
dc.contributor.institution | Univ Turin | - |
dc.description.affiliation | Univ Estadual Paulista UNESP, Fac Ciencias Farmaceut, Araraquara, SP, Brazil | - |
dc.description.affiliation | Univ Turin, Dipartimento Sci & Tecnol Farmaco, Turin, Italy | - |
dc.description.affiliationUnesp | Univ Estadual Paulista UNESP, Fac Ciencias Farmaceut, Araraquara, SP, Brazil | - |
dc.description.sponsorshipId | FAPESP: 12/50359-2 | - |
dc.description.sponsorshipId | FAPESP: 11/15520-4 | - |
dc.description.sponsorshipId | CAPES: 455903/2012-3 | - |
dc.description.sponsorshipId | CAPES: 310026/2011-3 | - |
dc.identifier.doi | 10.1128/AAC.00052-14 | - |
dc.identifier.wos | WOS:000339259200069 | - |
dc.rights.accessRights | Acesso restrito | - |
dc.identifier.file | WOS000339259200069.pdf | - |
dc.relation.ispartof | Antimicrobial Agents and Chemotherapy | - |
Appears in Collections: | Artigos, TCCs, Teses e Dissertações da Unesp |
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