Ruthenium (II) phosphine/picolinate complexes as antimycobacterial agents.
The synthesis, characterization and the anti-Mycobacterium tuberculosis (MTB) activities of three ruthenium complexes containing the 2-pyridinecarboxylic acid anion (picolinate), with formulae cis- [Ru(pic)(dppm)(2)]PF(6) (1), cis- [Ru(pic)(dppe)(2)]PF(6) (2) and [Ru(pic)(2)(PPh(3))(2)] (3) [pic=2-pyridinecarboxylate; dppm=bis(diphenylphosphino)methane; dppe=1,2-bis(diphenylphosphino)ethane; PPh(3)=triphenylphosphine] are reported in this article. The complexes were characterized by elemental analysis, spectroscopic and electrochemical techniques. Their in vitro antimycobacterial activity was determinated as the Minimum Inhibitory Concentration (MIC) for MTB cell growth, measured by the REMA method. The best MICs were found for complexes (1) and (2), with values of 0.78 and 0.26 microg/mL, respectively. The results are comparable to or better than "first line" or "second line" drugs commonly used in the treatment of TB.
Pavan
Fernando R
FR
Faculdade de Ciências Farmacêuticas, Universidade Estadual Paulista, CEP 14801-902, Araraquara, SP, Brazil. pavanfer@yahoo.com.br
Poelhsitz
Gustavo Von
GV
do Nascimento
Fábio B
FB
Leite
Sergio R A
SR
Batista
Alzir A
AA
Deflon
Victor M
VM
Sato
Daisy N
DN
Franzblau
Scott G
SG
Leite
Clarice Q F
CQ
D000900:Anti-Bacterial Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D004563:Electrochemistry; D004583:Electrons; D008024:Ligands; D008826:Microbial Sensitivity Tests; D009169:Mycobacterium tuberculosis / Q000187:drug effects; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D010720:Phosphines / Q000737:chemistry*; D010848:Picolinic Acids / Q000737:chemistry*; D012428:Ruthenium / Q000737:chemistry*
D000900:Anti-Bacterial Agents; D008024:Ligands; D009942:Organometallic Compounds; D010720:Phosphines; D010848:Picolinic Acids; D012428:Ruthenium; C044646:phosphine; C030614:picolinic acid