RHUTENIUM (II) PHOSPHINE/PICOLINATE COMPLEXES AS ANTIMYCOBACTERIAL AGENTS

Fernando Rogério Pavan (UNESP); Gustavo Von Poelhsitz (UFGO); Fabio B. do Nascimento (UFSCAR); Sergio Roberto de Andrade Leite (UNESP); Alzir A. Batista (UFSCAR); Victor M. Deflon (USP); Daisy Nakamura Sato (IAL); Scott Gary Franzblau (IUC); Clarice Queico Fujimura Leite (UNESP)

Introduction: The Mycobacterium tuberculosis (MTB), agent of tuberculosis is responsible for death around of 2-3 million people annually and for global economic toll of ~$12 billion each year. The rise of multidrug resistance (MDR) in MTB has complicated and extended the treatment. No new drugs have been developed specifically against mycobacteria since the 1960s and only within the last few years some promising drug candidates emerged. Thus, there is a great need to develop new therapeutics to treat tuberculosis to reduce the total duration of treatment and to provide more effective treatment for MDR TB and for latent tuberculosis infection. Objectives: The present work describes the anti-M. tuberculosis activities of three new ruthenium complexes (1, 2 and 3) containing the 2-pyridinecarboxylic acid anion, Material and Methods: The complexes were characterized by elemental analysis, spectroscopic and electrochemical techniques. The MIC of these complexes were investigated in order to determine their in vitro antimycobacterial activity against M. tuberculosis H₃₇Rv (ATCC 27294). The MIC values were determined using the REMA method (Microplate Rezarurin Assay). Results and Discussion: The best MIC were found for the complexes (1) and (2), which presented values of 0.78 and 0.26 μg/mL, respectively. From three new ruthenium (II) phosphine/picolinate complexes, synthesized, the ruthenium phosphine complexes (1) and (2) were qualified as potential antitubercular agents, better than some drugs commonly used in the TB treatment. Conclusion: Further studies should include the effect against drug-resistant strains and bacilli in a state of latency, as well as the intracellular evaluation of the new complexes.