Improving anti-trypanosomal activity of 3-aminoquinoxaline-2-carbonitrile N1,N4-dioxide derivatives by complexation with vanadium.
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.
Urquiola
Carolina
C
Cátedra de Química Inorgánica, DEC, Facultad de Química, Universidad de la República, Montevideo, Uruguay.
Vieites
Marisol
M
Aguirre
Gabriela
G
Marín
Adoración
A
Solano
Beatriz
B
Arrambide
Gabriel
G
Noblía
Pabla
P
Lavaggi
María Laura
ML
Torre
María H
MH
González
Mercedes
M
Monge
Antonio
A
Gambino
Dinorah
D
Cerecetto
Hugo
H
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*
D003497:Cyclic N-Oxides; D008024:Ligands; D011810:Quinoxalines; D014344:Trypanocidal Agents; D014639:Vanadium