期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 14, 期 16, 页码 5503-5509出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2006.04.041
关键词
anti-trypanosomal activity; quinoxaline N-1,N-4-dioxide; vanadium; N,O ligands
New vanadium complexes of the type [(VO)-O-IV(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. (c) 2006 Published by Elsevier Ltd.
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