title: Improving anti-trypanosomal activity of 3-aminoquinoxaline-2-carbonitrile N1,N4-dioxide derivatives by complexation with vanadium.
abstract: New vanadium complexes of the type [V(IV)O(L)(2)], where L are 3-aminoquinoxaline-2-carbonitrile N(1),N(4)-dioxide derivatives, were prepared as an effort to obtain new anti-trypanosomal agents improving the bioactivity of the free ligands. Complexation to vanadium of the quinoxaline ligands leads to excellent antiprotozoal activity, similar to that of the reference drugs nifurtimox and benznidazole and in all cases higher than that of the corresponding free ligands. In addition, it is for the first time that the V((IV))O-quinoxaline complexes are reported as a family of anti-Trypanosoma cruzi agents. Finally, the anti-trypanosomal activity of these vanadium complexes could be explained on the basis of their lipophilicity and the electronic characteristics of the quinoxaline substituents.
authors.affiliation: Cátedra de Química Inorgánica, DEC, Facultad de Química, Universidad de la República, Montevideo, Uruguay.
authors.forename: Carolina
authors.initials: C
authors.lastname: Urquiola
authors.forename: Marisol
authors.initials: M
authors.lastname: Vieites
authors.forename: Gabriela
authors.initials: G
authors.lastname: Aguirre
authors.forename: Adoración
authors.initials: A
authors.lastname: Marín
authors.forename: Beatriz
authors.initials: B
authors.lastname: Solano
authors.forename: Gabriel
authors.initials: G
authors.lastname: Arrambide
authors.forename: Pabla
authors.initials: P
authors.lastname: Noblía
authors.forename: María Laura
authors.initials: ML
authors.lastname: Lavaggi
authors.forename: María H
authors.initials: MH
authors.lastname: Torre
authors.forename: Mercedes
authors.initials: M
authors.lastname: González
authors.forename: Antonio
authors.initials: A
authors.lastname: Monge
authors.forename: Dinorah
authors.initials: D
authors.lastname: Gambino
authors.forename: Hugo
authors.initials: H
authors.lastname: Cerecetto
mesh_terms: D000818:Animals; D002478:Cells, Cultured; D003497:Cyclic N-Oxides / Q000737:chemistry / Q000494:pharmacology*; D008024:Ligands; D011810:Quinoxalines / Q000737:chemistry / Q000494:pharmacology*; D014344:Trypanocidal Agents / Q000737:chemistry / Q000494:pharmacology*; D014349:Trypanosoma cruzi / Q000187:drug effects* / Q000378:metabolism; D014639:Vanadium / Q000737:chemistry*
chemical_list: D003497:Cyclic N-Oxides; D008024:Ligands; D011810:Quinoxalines; D014344:Trypanocidal Agents; D014639:Vanadium