New isoniazid complexes, promising agents against mycobacterium tuberculosis

Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP)

Processo FAPESP: 09/06499-1

Processo FAPESP: 11/11593-7

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.