Improving anti-trypanosomal activity of 3-aminoquinoxaline-2-carbonitrile N1,N4-dioxide derivatives by complexation with vanadium

New vanadium complexes of the type [VIVO(L)2], where L are 3-aminoquinoxaline-2-carbonitrile N1,N4-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.

New vanadium complexes of the type [VIVO(L)2], where L are 3-aminoquinoxaline-2-carbonitrile N1,N4-dioxide derivatives, are described. Complexation to vanadium of the quinoxaline ligands leads to excellent antiprotozoal agents. Anti-Trypanosoma cruzi activity is explained on the basis of lipophilicity and electronic properties of quinoxaline substituents.Figure optionsDownload as PowerPoint slide