Chemistry
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Item The antimalarial activity of Ru?chloroquine complexes against resistant Plasmodium falciparum is related to lipophilicity, basicity, and heme aggregation inhibition ability near water/n-octanol interfaces(Journal of Biological Inorganic Chemistry, 2009) Martínez, A.; Rajapakse, C.S.K.; Jalloh, D.; Dautriche, C.; Sánchez-Delgado, R.A.We have measured water/n-octanol partition coefficients, pK a values, heme binding constants, and heme aggregation inhibition activity of a series of ruthenium??-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.