New isoniazid complexes, promising agents against mycobacterium tuberculosis
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Data
2013-07-01
Autores
Poggi, Mariana
Barroso, Rafael
Costa-Filho, Antonio José
De Barros, Heloisa Barbosa [UNESP]
Pavan, Fernando [UNESP]
Leite, Clarice Queico [UNESP]
Gambino, Dinorah
Torre, María Helvecia
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Resumo
Tuberculosis (TB) is a public health disease that produces several million deaths annually worldwide. Due to this critical situation and the appearance of drug-resistant microbial strains, innovation in TB drug discovery is a research priority. In this work, the synthesis and characterization by elemental analysis, thermogravimetry, conductimetric measurements and spectroscopies UV-Vis, IR and EPR of [Cu(INH)(H2O)]SO4·2H2O (Cu-INH) and [CoCl(INH)2(H2O)] Cl·2.5H2O (Co-INH) complexes with isoniazid (INH) are reported. Besides, the lipophilicity, the activity against Mycobacterium tuberculosis (MICCu-INH = 0.78 μg/mL and MICCo-INH = 0.19 μg/mL) and the cytotoxicity (IC50 = 48.8 and 625 μg/mL for the copper and cobalt complexes, respectively) were measured and the selectivity index (62.5 for Cu-INH and 3205 for Co-INH) was calculated. These results indicate that these complexes are good candidates for further studies. © 2013, Sociedad Química de México.
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Antimycobacteria activity, Copper and cobalt complexes, Isoniazid, Spectroscopy, Tuberculosis
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Journal of the Mexican Chemical Society, v. 57, n. 3, p. 198-204, 2013.