Bioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents

dc.contributorCátedra de Química Inorgánica, Departamento Estrella Campos, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay.
dc.contributorUniversidade Estadual Paulista (Unesp)
dc.contributorDepartamento de Física, Facultad de Ciencias Exactas, Universidad Nacional de La Plata and IFLP (CONICET, CCT-La Plata), C.C. 67, 1900 La Plata, Argentina.
dc.contributorCátedra de Química Inorgánica, Departamento Estrella Campos, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay. Electronic address: dgambino@fq.edu.uy.
dc.creatorMachado, Ignacio
dc.creatorMarino, Leonardo Biancolino [UNESP]
dc.creatorDemoro, Bruno
dc.creatorEcheverría, Gustavo A.
dc.creatorPiro, Oscar E.
dc.creatorLeite, Clarice Q. F. [UNESP]
dc.creatorPavan, Fernando R. [UNESP]
dc.creatorGambino, Dinorah
dc.date2015-12-07T15:31:18Z
dc.date2015-12-07T15:31:18Z
dc.date2014-11-24
dc.date.accessioned2023-09-12T07:28:41Z
dc.date.available2023-09-12T07:28:41Z
dc.identifierhttp://dx.doi.org/10.1016/j.ejmech.2014.09.067
dc.identifierEuropean Journal Of Medicinal Chemistry, v. 87, p. 267-273, 2014.
dc.identifier1768-3254
dc.identifierhttp://hdl.handle.net/11449/131065
dc.identifier10.1016/j.ejmech.2014.09.067
dc.identifier25261824
dc.identifier.urihttps://repositorioslatinoamericanos.uchile.cl/handle/2250/8780346
dc.descriptionIn 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(III)(mpo)3] complexes, with M = Ga or Bi, were synthesized and characterized in the solid state and in solution. Attempts to crystallize [Ga(III)(mpo)3] in CH2Cl2 led to single crystals of the reaction product [GaCl(mpo)2], 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(III)(mpo)3] 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 H37Rv ATCC 27294 (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.
dc.descriptionCátedra de Química Inorgánica, Departamento Estrella Campos, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay.
dc.descriptionFacultade de Ciencias Farmacêuticas, UNESP, 14801-902 Araraquara, SP, Brazil.
dc.descriptionDepartamento de Física, Facultad de Ciencias Exactas, Universidad Nacional de La Plata and IFLP (CONICET, CCT-La Plata), C.C. 67, 1900 La Plata, Argentina.
dc.descriptionCátedra de Química Inorgánica, Departamento Estrella Campos, Facultad de Química, Universidad de la República, Gral. Flores 2124, 11800 Montevideo, Uruguay. Electronic address: dgambino@fq.edu.uy.
dc.descriptionFacultade de Ciencias Farmacêuticas, UNESP, 14801-902 Araraquara, SP, Brazil.
dc.format267-273
dc.languageeng
dc.publisherElsevier B. V.
dc.relationEuropean Journal Of Medicinal Chemistry
dc.rightsAcesso restrito
dc.sourcePubMed
dc.subjectBismuth(iii)
dc.subjectGallium(iii)
dc.subjectIron(iii)
dc.subjectMycobacterium tuberculosis
dc.subjectPyridine-2-thiol 1-oxide compounds
dc.titleBioactivity of pyridine-2-thiolato-1-oxide metal complexes: Bi(III), Fe(III) and Ga(III) complexes as potent anti-Mycobacterium tuberculosis prospective agents
dc.typeArtigo


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