New Isoniazid Complexes, Promising Agents Against Mycobacterium tuberculosis

Author(s)

Poggi, Mariana ^[1] ; Barroso, Rafael ^[2] ; Costa-Filho, Antonio Jose ^[2] ; de Barros, Heloisa Barbosa ^[3] ; Pavan, Fernando ^[3] ; Leite, Clarice Queico ^[3] ; Gambino, Dinorah ^[1] ; Helvecia Torre, Maria ^[1]

Affiliation

^[1] Univ Republica, Fac Quim, Catedra Quim Inorgan, Montevideo 11800 - Uruguay

^[2] Univ Sao Paulo, Fac Filosofia Ciencias & Letras Ribeirao Preto, BR-14040901 Ribeirao Preto, SP - Brazil

^[3] Univ Estadual Paulista, UNESP, Fac Ciencias Farmaceut, Dept Ciencias Biol, BR-14801902 Araraquara, SP - Brazil

• Document type: Journal article
• Source: Journal of the Mexican Chemical Society; v. 57, n. 3, p. 198-204, JUL-SEP 2013.
• Web of Science Citations: 13

Abstract

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 (MIC Cu-INH = 0.78 µg/mL and MIC Co-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. (AU)

• FAPESP's process: 11/11593-7 - Research for new drugs against tuberculosis: laboratory improvement to perform pre-clinical trials
• Grantee: Fernando Rogério Pavan
• Support Opportunities: Scholarships in Brazil - Post-Doctoral
• FAPESP's process: 09/06499-1 - Determination of in vitro and in vivo anti-tuberculosis activity of phosphines/diimines Ru (II) complexes
• Grantee: Clarice Queico Fujimura Leite
• Support Opportunities: Regular Research Grants