title: Antileishmanial activity of ruthenium(II)tetraammine nitrosyl complexes.
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.
authors.affiliation: Departamento de Química e Física Molecular, Instituto de Química de São Carlos-Universidade de São Paulo, São Carlos, SP, Brazil.
authors.forename: José Clayston Melo
authors.initials: JC
authors.lastname: Pereira
authors.forename: Vanessa
authors.initials: V
authors.lastname: Carregaro
authors.forename: Diego Luís
authors.initials: DL
authors.lastname: Costa
authors.forename: João Santana
authors.initials: JS
authors.lastname: da Silva
authors.forename: Fernando Q
authors.initials: FQ
authors.lastname: Cunha
authors.forename: Douglas Wagner
authors.initials: DW
authors.lastname: Franco
mesh_terms: D000818:Animals; D000981:Antiprotozoal Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D020128:Inhibitory Concentration 50; D018320:Leishmania major / Q000166:cytology / Q000187:drug effects* / Q000502:physiology; D016773:Leishmaniasis, Cutaneous / Q000188:drug therapy; D008264:Macrophages / Q000187:drug effects / Q000378:metabolism; D051379:Mice; D008807:Mice, Inbred BALB C; D009569:Nitric Oxide / Q000378:metabolism; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology* / Q000627:therapeutic use; D012428:Ruthenium / Q000737:chemistry*; D013237:Stereoisomerism
chemical_list: D000981:Antiprotozoal Agents; D009942:Organometallic Compounds; D009569:Nitric Oxide; D012428:Ruthenium