Reversed chloroquines based on the 3,4-dihydropyrimidin-2(1H)-one scaffold: synthesis and evaluation for antimalarial, beta-haematin inhibition, and cytotoxic activity.
Natasha October;
Nicholas D Watermeyer;
Vanessa Yardley;
Timothy J Egan;
Kanyile Ncokazi;
Kelly Chibale;
(2008)
Reversed chloroquines based on the 3,4-dihydropyrimidin-2(1H)-one scaffold: synthesis and evaluation for antimalarial, beta-haematin inhibition, and cytotoxic activity.
ChemMedChem, 3 (11).
pp. 1649-1653.
ISSN 1860-7179
DOI: 10.1002/cmdc.200800172
(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.
| Item Type | Article |
|---|---|
| Keywords | drug design, quinoline-containing antimalarials, dihydropyrimidinones, reversing agents, sensitizers, PLASMODIUM-FALCIPARUM, DRUG-RESISTANCE, MALARIA, ANTAGONISTS |
| ISI | 261359400003 |