Ruthenium(II) complexes with hydroxypyridinecarboxylates: Screening potential metallodrugs against Mycobacterium tuberculosis. (8th January 2015) - Barbosa, Marília I.F.
Graphical abstract: Three new promising antimycobacterium tuberculosis ruthenium(II) complexes with the anions of 2-hydroxynicotinic acid (2-OHnicH), 6-hydroxynicotinic acid (6-OHnicH) and 3-hydroxypicolinic acid (3-OHpicH) were synthesized and characterized. Abstract: Three promising antimycobacterium tuberculosis ruthenium(II) complexes with the deprotonated ligands 2-hydroxynicotinic acid (2-OHnicH), 6-hydroxynicotinic acid (6-OHnicH) and 3-hydroxypicolinic acid (3-OHpicH) were synthesized and characterized. Structural analysis revealed three different coordination modes depending of the hydroxypyridinecarboxylate ligand. In the complex [Ru(2-OHnic)(dppb)(bipy)]PF6 (1 ), the 2-OHnic anion is coordinated by the O, O-chelating mode (via carboxylate group and phenolate oxygen), in the [Ru(6-OHnic)(dppb)(bipy)]PF6 (2 ) a O–O chelation by the carboxylate group is observed for the 6-OHnic ligand and for the complex [Ru(3-OHpic)(dppb)(bipy)]PF6 (3 ) a N, O-chelating mode (via carboxylate) occurs to the 3-OHpic anion. The compounds were evaluated for activity against Mycobacterium tuberculosis H37 Rv ATCC 27294 using Resazurin Microtitre Assay (REMA) plate method and cytotoxicity in VERO CCL-81 cell line. All the synthesized compounds exhibited good antimycobacterial activity and a completely lack of cytotoxicity activity, indicating a good selectivity index.