Antileishmanial activity of ruthenium(II)tetraammine nitrosyl complexes.

Authors :: Pereira JC
Carregaro V
Costa DL
da Silva JS
Cunha FQ
Franco DW
Source :: European journal of medicinal chemistry [Eur J Med Chem] 2010 Sep; Vol. 45 (9), pp. 4180-7. Date of Electronic Publication: 2010 Jun 12.
Publication Year :: 2010
Abstract: The complexes trans-[Ru(NO)(NH(3))(4)L](X)(3) (X = BF(4)(-), PF(6)(-) or Cl(-) and L = N-heterocyclic ligands, P(OEt)(3), SO(3)(-2)), and [Ru(NO)Hedta)] were shown to exhibit IC(50pro) in the range of 36 (L = imN) to 5000 microM (L = imC). The inhibitory effects of trans-[Ru(NO)(NH(3))(4)imN](BF(4))(3) and of the Angeli's salt on the growth of the intramacrophage amastigote form studied were found to be similar while the trans-[Ru(NH(3))(4)imN(H(2)O)](2+) complex was found not to exhibit any substantial antiamastigote effect. The trans-[Ru(NO)(NH(3))(4)imN](BF(4))(3) compound, administered (500 nmol kg(-1) day(-1)) in BALB/c mice infected with Leishmania major, was found to exhibit a 98% inhibition on the parasite growth. Furthermore, this complex proved to be at least 66 times more efficient than glucantime in in vivo experiments.<br /> (2010 Elsevier Masson SAS. All rights reserved.)