期刊
JOURNAL OF BIOLOGICAL INORGANIC CHEMISTRY
卷 14, 期 6, 页码 863-871出版社
SPRINGER
DOI: 10.1007/s00775-009-0498-4
关键词
Chloroquine; Ruthenium; Malaria; Heme aggregation; Lipophilicity
资金
- NIH [1S06GM 076168-04, MARC GM08078]
We have measured water/n-octanol partition coefficients, pK (a) values, heme binding constants, and heme aggregation inhibition activity of a series of ruthenium-pi-arene-chloroquine (CQ) complexes recently reported to be active against CQ-resistant strains of Plasmodium falciparum. Measurements of heme aggregation inhibition activity of the metal complexes near water/n-octanol interfaces qualitatively predict their superior antiplasmodial action against resistant parasites, in relation to CQ; we conclude that this modified method may be a better predictor of antimalarial potency than standard tests in aqueous acidic buffer. Some interesting tendencies emerge from our data, indicating that the antiplasmodial activity is related to a balance of effects associated with the lipophilicity, basicity, and structural details of the compounds studied.
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