Ruthenium(II) complexes with hydroxypyridinecarboxylates: Screening potential metallodrugs against Mycobacterium tuberculosis

Author(s)

Barbosa, Marilia I. F. ^[1] ; Correa, Rodrigo S. ^[1] ; Pozzi, Lucas V. ^[1] ; Lopes, Erica de O. ^[2] ; Pavan, Fernando R. ^[2] ; Leite, Clarice Q. F. ^[2] ; Ellena, Javier ^[3] ; Machado, Sergio de P. ^[4] ; Von Poelhsitz, Gustavo ^[5] ; Batista, Alzir A. ^[1]

Affiliation

^[1] Univ Fed Sao Carlos, Dept Quim, BR-13565905 Sao Carlos, SP - Brazil

^[2] Univ Estadual Paulista, Dept Ciencias Biol, Fac Ciencias Farmaceut, BR-14800900 Araraquara, SP - Brazil

^[3] Univ Sao Paulo, Inst Fis Sao Carlos, BR-13560970 Sao Carlos, SP - Brazil

^[4] Univ Fed Rio de Janeiro, Inst Quim, BR-21941590 Rio De Janeiro, RJ - Brazil

^[5] Univ Fed Uberlandia, Inst Quim, BR-38400902 Uberlandia, MG - Brazil

• Document type: Journal article
• Source: Polyhedron; v. 85, p. 376-382, JAN 8 2015.
• Web of Science Citations: 17

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 H(37)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. (C) 2014 Elsevier Ltd. All rights reserved. (AU)

• FAPESP's process: 13/26559-4 - Structural modifications in biologically active Ru(II) complexes toward the design of new metallodrug candidates
• Grantee: Rodrigo de Souza Corrêa
• Support Opportunities: Scholarships in Brazil - Post-Doctoral