Reversed chloroquines based on the 3,4-dihydropyrimidin-2(1H)-one scaffold: synthesis and evaluation for antimalarial, beta-haematin inhibition, and cytotoxic activity.

(Chemical Equation Presented) The synthesis, cytotoxicity, and antimalarial activity of resistance-reversing bifunctional dihydropyrimidone-chloroquinoline conjugates are reported herein. In vitro assay results indicate this class of compounds is highly active against both chloroquine-resistant and chloroquine-sensitive strains of P. falciparum. © 2008 Wiley-VCH Verlag GmbH & Co. KGaA.