期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 60, 期 -, 页码 64-75出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2012.11.038
关键词
N-heterocyclic carbene; Silver; Gold; Organometallic complexes; Antiplasmodial drugs
资金
- Centre National de la Recherche Scientifique (CNRS)
- University Paul Sabatier Toulouse (BQR grant)
A series of mono-and dinuclear silver(I) and mononuclear gold(I) complexes containing bis(N-hetero-cyclic carbene) (NHC) or N-functionalized NHC ligands were synthesized and fully characterized by spectroscopic methods and, in some cases, by single crystal X-ray diffraction. The in vitro antiplasmodial and antifungal activities of a previously described family of N-functionalized bis(imidazolium) proligands and their corresponding silver(I), gold(I) and gold(III) complexes but also the new here described compounds were investigated in a chloroquine-resistant strain of Plasmodium falciparum, and against two Candida strains, respectively. For the first family, interesting antiplasmodial and antifungal activities were found for the dinuclear silver(I) species but they also showed strong hemolytic properties. Pharmaco-modulations leading to the second series of complexes allowed notably increase in the antiplasmodial activity, in particular of the mononuclear gold(I) complexes with IC50 values up to. 330 nM, without any hemolysis. (C) 2012 Published by Elsevier Masson SAS.
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