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(s): 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
• Date: 2018
• Persistent ID: http://hdl.handle.net/11449/177243
• Origin: Oasisbr
• Subject(s): Bismuth(III); Gallium(III); Iron(III); Mycobacterium tuberculosis; Pyridine-2-thiol 1-oxide compounds
• Document Type: Journal article
• Language: English

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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^III(mpo)3] complexes, withM Combining double low line Ga or Bi, were synthesized and characterized in the solid state and in solution. Attempts to crystallize [Ga^III(mpo)3] in CH2Cl2led 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 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 2124

Facultade de Ciencias Farmacêuticas, UNESP

Departamento de Física, Universidad Nacional de la Plata, IFLP, C.C. 67

Facultade de Ciencias Farmacêuticas, UNESP