Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives
Autor(a) principal: | |
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Data de Publicação: | 2010 |
Outros Autores: | , , , , , |
Tipo de documento: | Artigo |
Idioma: | eng |
Título da fonte: | Repositório Institucional da FIOCRUZ (ARCA) |
Texto Completo: | https://www.arca.fiocruz.br/handle/icict/37441 |
Resumo: | 2020-11-28 |
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Gonçalves, Raoni S. B.Kaiser, Carlos R.Lourenço, Maria C. S.Souza, Marcus V. N. deWardell, James L.Wardell, Solange M. S. V.Silva, Adilson D. da2019-11-28T13:03:41Z2019-11-28T13:03:41Z2010GONÇALVES, Raoni S. B. et al. Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives. European Journal of Medicinal Chemistry, v. 45, p. 6095-6100, 2010.0223-5234https://www.arca.fiocruz.br/handle/icict/3744110.1016/j.ejmech.2010.09.0241768-3254engElsevierSynthesis and antitubercular activity of new mefloquine-oxazolidine derivativesinfo:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article2020-11-28Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil / Universidade Federal do Rio de Janeiro. Instituto de Química. Programa de Pós-Graduação em Química. Rio de Janeiro, RJ, Brasil.Universidade Federal do Rio de Janeiro. Instituto de Química. Programa de Pós-Graduação em Química. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Pesquisas Clínica Evandro Chagas. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Instituto de Tecnologia em Fármacos. Rio de Janeiro, RJ, Brasil / Universidade Federal do Rio de Janeiro. Instituto de Química. Programa de Pós-Graduação em Química. Rio de Janeiro, RJ, Brasil.Fundação Oswaldo Cruz. Centro de Desenvolvimento Tecnológico em Saúde. Rio de Janeiro, RJ, Brasil.CHEMSOL. Aberdeen, Scotland, UK.Universidade Federal de Juiz de Fora. Instituto de Ciências Exatas. Departamento de Química. Juiz de Fora, MG, Brasil.In this work, we report the synthesis and the antitubercular evaluation of 16 new mefloquine derivatives, formed from reactions between mefloquine and benzaldehydes, with the activity expressed as the minimum inhibitory concentration (MIC) in mM. The compounds were non-cytotoxic and exhibited an important activity (12.6 mM). The appreciable activity of these compounds can be considered an important finding for the rational design of new leads for anti-TB compounds.TuberculosisQuinolineMefloquineinfo:eu-repo/semantics/openAccessreponame:Repositório Institucional da FIOCRUZ (ARCA)instname:Fundação Oswaldo Cruz (FIOCRUZ)instacron:FIOCRUZLICENSElicense.txttext/plain1748https://www.arca.fiocruz.br/bitstream/icict/37441/1/license.txt8a4605be74aa9ea9d79846c1fba20a33MD51ORIGINALve_Gonçalves_Raoni_etal_INI_2010.pdfve_Gonçalves_Raoni_etal_INI_2010.pdfapplication/pdf433365https://www.arca.fiocruz.br/bitstream/icict/37441/2/ve_Gon%c3%a7alves_Raoni_etal_INI_2010.pdf89dcc56795d2a4f7e727ad7c429a29e2MD52TEXTve_Gonçalves_Raoni_etal_INI_2010.pdf.txtve_Gonçalves_Raoni_etal_INI_2010.pdf.txtExtracted texttext/plain36388https://www.arca.fiocruz.br/bitstream/icict/37441/3/ve_Gon%c3%a7alves_Raoni_etal_INI_2010.pdf.txtd7f0588681660163d48a41ffd445a3f4MD53icict/374412021-03-24 16:32:40.134oai:www.arca.fiocruz.br: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Repositório InstitucionalPUBhttps://www.arca.fiocruz.br/oai/requestrepositorio.arca@fiocruz.bropendoar:21352021-03-24T19:32:40Repositório Institucional da FIOCRUZ (ARCA) - Fundação Oswaldo Cruz (FIOCRUZ)false |
dc.title.pt_BR.fl_str_mv |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
title |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
spellingShingle |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives Gonçalves, Raoni S. B. Tuberculosis Quinoline Mefloquine |
title_short |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
title_full |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
title_fullStr |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
title_full_unstemmed |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
title_sort |
Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives |
author |
Gonçalves, Raoni S. B. |
author_facet |
Gonçalves, Raoni S. B. Kaiser, Carlos R. Lourenço, Maria C. S. Souza, Marcus V. N. de Wardell, James L. Wardell, Solange M. S. V. Silva, Adilson D. da |
author_role |
author |
author2 |
Kaiser, Carlos R. Lourenço, Maria C. S. Souza, Marcus V. N. de Wardell, James L. Wardell, Solange M. S. V. Silva, Adilson D. da |
author2_role |
author author author author author author |
dc.contributor.author.fl_str_mv |
Gonçalves, Raoni S. B. Kaiser, Carlos R. Lourenço, Maria C. S. Souza, Marcus V. N. de Wardell, James L. Wardell, Solange M. S. V. Silva, Adilson D. da |
dc.subject.en.pt_BR.fl_str_mv |
Tuberculosis Quinoline Mefloquine |
topic |
Tuberculosis Quinoline Mefloquine |
description |
2020-11-28 |
publishDate |
2010 |
dc.date.issued.fl_str_mv |
2010 |
dc.date.accessioned.fl_str_mv |
2019-11-28T13:03:41Z |
dc.date.available.fl_str_mv |
2019-11-28T13:03:41Z |
dc.type.status.fl_str_mv |
info:eu-repo/semantics/publishedVersion |
dc.type.driver.fl_str_mv |
info:eu-repo/semantics/article |
format |
article |
status_str |
publishedVersion |
dc.identifier.citation.fl_str_mv |
GONÇALVES, Raoni S. B. et al. Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives. European Journal of Medicinal Chemistry, v. 45, p. 6095-6100, 2010. |
dc.identifier.uri.fl_str_mv |
https://www.arca.fiocruz.br/handle/icict/37441 |
dc.identifier.issn.pt_BR.fl_str_mv |
0223-5234 |
dc.identifier.doi.none.fl_str_mv |
10.1016/j.ejmech.2010.09.024 |
dc.identifier.eissn.none.fl_str_mv |
1768-3254 |
identifier_str_mv |
GONÇALVES, Raoni S. B. et al. Synthesis and antitubercular activity of new mefloquine-oxazolidine derivatives. European Journal of Medicinal Chemistry, v. 45, p. 6095-6100, 2010. 0223-5234 10.1016/j.ejmech.2010.09.024 1768-3254 |
url |
https://www.arca.fiocruz.br/handle/icict/37441 |
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eng |
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eng |
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info:eu-repo/semantics/openAccess |
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openAccess |
dc.publisher.none.fl_str_mv |
Elsevier |
publisher.none.fl_str_mv |
Elsevier |
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reponame:Repositório Institucional da FIOCRUZ (ARCA) instname:Fundação Oswaldo Cruz (FIOCRUZ) instacron:FIOCRUZ |
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Fundação Oswaldo Cruz (FIOCRUZ) |
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FIOCRUZ |
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FIOCRUZ |
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