Reversed Chloroquines Based on the 3,4-Dihydropyrimidin-2(1H)-one Scaffold: Synthesis and Evaluation for Antimalarial, b-Haematin Inhibition, and Cytotoxic Activity

Reversed Chloroquines Based on the 3,4-Dihydropyrimidin-2(1H)-one Scaffold: Synthesis and Evaluation for Antimalarial, b-Haematin Inhibition, and Cytotoxic Activity

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...

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Bibliographic Details
Published in:ChemMedChem Vol. 3; no. 11; pp. 1649 - 1653
Main Authors: October, Natasha, Watermeyer, Nicholas D, Yardley, Vanessa, Egan, Timothy J, Ncokazi, Kanyile, Chibale, Kelly
Format: Journal Article
Language:German
Published: 17-11-2008
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Summary: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.
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ISSN:1860-7179
DOI:10.1002/cmdc.200800172