Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents
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Publication Date: | 2014 |
Other Authors: | , , , , , , |
Format: | Article |
Language: | eng |
Source: | Repositório Institucional da UNESP |
Download full: | http://dx.doi.org/10.2217/ebo.12.500 http://hdl.handle.net/11449/177243 |
Summary: | In the search for new therapeutic tools against tuberculosis and to further address the therapeutic potential of pyridine-2-thiol 1-oxide (Hmpo) metal complexes, two new octahedral [M<sup>III</sup>(mpo)<inf>3</inf>] complexes, withM Combining double low line Ga or Bi, were synthesized and characterized in the solid state and in solution. Attempts to crystallize [Ga<sup>III</sup>(mpo)<inf>3</inf>] in CH<inf>2</inf>Cl<inf>2</inf>led to single crystals of the reaction product [GaCl(mpo)<inf>2</inf>], where the gallium(III) ion is in a square basis pyramidal environment, trans-coordinated at the basis to two pyridine-2-thiolato 1-oxide anions acting as bidentate ligands through their oxygen and sulfur atoms.The biological activity of the new [M<sup>III</sup>(mpo)<inf>3</inf>] complexes together with that of the previously reported Fe(III) analogous compound and the pyridine-2-thiol 1-oxide sodium salt (Na mpo) was evaluated on Mycobacterium tuberculosis. The compounds showed excellent activity, both in the standard strain H<inf>37</inf>Rv ATCC27294 (pan-susceptible) and in five clinical isolates that are resistant to the standard first-line anti-tuberculosis drugs isoniazid and rifampicin. These pyridine-2-thiol 1-oxide derivatives are promising compounds for the treatment of resistant tuberculosis. |
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Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agentsBismuth(III)Gallium(III)Iron(III)Mycobacterium tuberculosisPyridine-2-thiol 1-oxide compoundsIn the search for new therapeutic tools against tuberculosis and to further address the therapeutic potential of pyridine-2-thiol 1-oxide (Hmpo) metal complexes, two new octahedral [M<sup>III</sup>(mpo)<inf>3</inf>] complexes, withM Combining double low line Ga or Bi, were synthesized and characterized in the solid state and in solution. Attempts to crystallize [Ga<sup>III</sup>(mpo)<inf>3</inf>] in CH<inf>2</inf>Cl<inf>2</inf>led to single crystals of the reaction product [GaCl(mpo)<inf>2</inf>], where the gallium(III) ion is in a square basis pyramidal environment, trans-coordinated at the basis to two pyridine-2-thiolato 1-oxide anions acting as bidentate ligands through their oxygen and sulfur atoms.The biological activity of the new [M<sup>III</sup>(mpo)<inf>3</inf>] complexes together with that of the previously reported Fe(III) analogous compound and the pyridine-2-thiol 1-oxide sodium salt (Na mpo) was evaluated on Mycobacterium tuberculosis. The compounds showed excellent activity, both in the standard strain H<inf>37</inf>Rv ATCC27294 (pan-susceptible) and in five clinical isolates that are resistant to the standard first-line anti-tuberculosis drugs isoniazid and rifampicin. These pyridine-2-thiol 1-oxide derivatives are promising compounds for the treatment of resistant tuberculosis.Cátedra de Química Inorgánica, Departamento Estrella Campos, Universidad de la República, Gral. Flores 2124Facultade de Ciencias Farmacêuticas, UNESPDepartamento de Física, Universidad Nacional de la Plata, IFLP, C.C. 67Facultade de Ciencias Farmacêuticas, UNESPCátedra de Química Inorgánica, Departamento Estrella Campos, Universidad de la RepúblicaUniversidade Estadual Paulista (Unesp)MacHado, IgnacioMarino, Leonardo Biancolino [UNESP]Demoro, BrunoEcheverría, Gustavo A.Piro, Oscar E.Leite, Clarice Q.F. [UNESP]Pavan, Fernando R. [UNESP]Gambino, Dinorah2018-12-11T17:24:36Z2018-12-11T17:24:36Z2014-11-24info:eu-repo/semantics/publishedVersioninfo:eu-repo/semantics/article267-273application/pdfhttp://dx.doi.org/10.2217/ebo.12.500European Journal of Medicinal Chemistry, v. 87, p. 267-273.1768-32540223-5234http://hdl.handle.net/11449/17724310.2217/ebo.12.5002-s2.0-849075784662-s2.0-84907578466.pdfScopusreponame:Repositório Institucional da UNESPinstname:Universidade Estadual Paulista (UNESP)instacron:UNESPengEuropean Journal of Medicinal Chemistry1,266info:eu-repo/semantics/openAccess2024-01-19T06:29:15Zoai:repositorio.unesp.br:11449/177243Repositório InstitucionalPUBhttp://repositorio.unesp.br/oai/requestopendoar:29462024-01-19T06:29:15Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP)false |
dc.title.none.fl_str_mv |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
title |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
spellingShingle |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents MacHado, Ignacio Bismuth(III) Gallium(III) Iron(III) Mycobacterium tuberculosis Pyridine-2-thiol 1-oxide compounds |
title_short |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
title_full |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
title_fullStr |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
title_full_unstemmed |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
title_sort |
Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents |
author |
MacHado, Ignacio |
author_facet |
MacHado, Ignacio Marino, Leonardo Biancolino [UNESP] Demoro, Bruno Echeverría, Gustavo A. Piro, Oscar E. Leite, Clarice Q.F. [UNESP] Pavan, Fernando R. [UNESP] Gambino, Dinorah |
author_role |
author |
author2 |
Marino, Leonardo Biancolino [UNESP] Demoro, Bruno Echeverría, Gustavo A. Piro, Oscar E. Leite, Clarice Q.F. [UNESP] Pavan, Fernando R. [UNESP] Gambino, Dinorah |
author2_role |
author author author author author author author |
dc.contributor.none.fl_str_mv |
Cátedra de Química Inorgánica, Departamento Estrella Campos, Universidad de la República Universidade Estadual Paulista (Unesp) |
dc.contributor.author.fl_str_mv |
MacHado, Ignacio Marino, Leonardo Biancolino [UNESP] Demoro, Bruno Echeverría, Gustavo A. Piro, Oscar E. Leite, Clarice Q.F. [UNESP] Pavan, Fernando R. [UNESP] Gambino, Dinorah |
dc.subject.por.fl_str_mv |
Bismuth(III) Gallium(III) Iron(III) Mycobacterium tuberculosis Pyridine-2-thiol 1-oxide compounds |
topic |
Bismuth(III) Gallium(III) Iron(III) Mycobacterium tuberculosis Pyridine-2-thiol 1-oxide compounds |
description |
In the search for new therapeutic tools against tuberculosis and to further address the therapeutic potential of pyridine-2-thiol 1-oxide (Hmpo) metal complexes, two new octahedral [M<sup>III</sup>(mpo)<inf>3</inf>] complexes, withM Combining double low line Ga or Bi, were synthesized and characterized in the solid state and in solution. Attempts to crystallize [Ga<sup>III</sup>(mpo)<inf>3</inf>] in CH<inf>2</inf>Cl<inf>2</inf>led to single crystals of the reaction product [GaCl(mpo)<inf>2</inf>], where the gallium(III) ion is in a square basis pyramidal environment, trans-coordinated at the basis to two pyridine-2-thiolato 1-oxide anions acting as bidentate ligands through their oxygen and sulfur atoms.The biological activity of the new [M<sup>III</sup>(mpo)<inf>3</inf>] complexes together with that of the previously reported Fe(III) analogous compound and the pyridine-2-thiol 1-oxide sodium salt (Na mpo) was evaluated on Mycobacterium tuberculosis. The compounds showed excellent activity, both in the standard strain H<inf>37</inf>Rv ATCC27294 (pan-susceptible) and in five clinical isolates that are resistant to the standard first-line anti-tuberculosis drugs isoniazid and rifampicin. These pyridine-2-thiol 1-oxide derivatives are promising compounds for the treatment of resistant tuberculosis. |
publishDate |
2014 |
dc.date.none.fl_str_mv |
2014-11-24 2018-12-11T17:24:36Z 2018-12-11T17:24:36Z |
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.uri.fl_str_mv |
http://dx.doi.org/10.2217/ebo.12.500 European Journal of Medicinal Chemistry, v. 87, p. 267-273. 1768-3254 0223-5234 http://hdl.handle.net/11449/177243 10.2217/ebo.12.500 2-s2.0-84907578466 2-s2.0-84907578466.pdf |
url |
http://dx.doi.org/10.2217/ebo.12.500 http://hdl.handle.net/11449/177243 |
identifier_str_mv |
European Journal of Medicinal Chemistry, v. 87, p. 267-273. 1768-3254 0223-5234 10.2217/ebo.12.500 2-s2.0-84907578466 2-s2.0-84907578466.pdf |
dc.language.iso.fl_str_mv |
eng |
language |
eng |
dc.relation.none.fl_str_mv |
European Journal of Medicinal Chemistry 1,266 |
dc.rights.driver.fl_str_mv |
info:eu-repo/semantics/openAccess |
eu_rights_str_mv |
openAccess |
dc.format.none.fl_str_mv |
267-273 application/pdf |
dc.source.none.fl_str_mv |
Scopus reponame:Repositório Institucional da UNESP instname:Universidade Estadual Paulista (UNESP) instacron:UNESP |
instname_str |
Universidade Estadual Paulista (UNESP) |
instacron_str |
UNESP |
institution |
UNESP |
reponame_str |
Repositório Institucional da UNESP |
collection |
Repositório Institucional da UNESP |
repository.name.fl_str_mv |
Repositório Institucional da UNESP - Universidade Estadual Paulista (UNESP) |
repository.mail.fl_str_mv |
|
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1799965663641468928 |