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

Reversed Chloroquines Based on the 3,4‐Dihydropyrimidin‐2(1H)‐one Scaffold: Synthesis and Evaluation for Antimalarial, β‐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:English
Published: Weinheim WILEY‐VCH Verlag 17-11-2008
Subjects:
Animals
Antimalarials - pharmacology
Chemistry, Pharmaceutical - methods
Chloroquine - chemistry
Chloroquine - pharmacology
dihydropyrimidinones
Drug Design
Hemeproteins - antagonists & inhibitors
Inhibitory Concentration 50
Magnetic Resonance Spectroscopy
Models, Biological
Models, Chemical
Molecular Structure
Pyrimidines - chemical synthesis
Pyrimidines - metabolism
quinoline‐containing antimalarials
reversing agents
sensitizers
Structure-Activity Relationship
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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.
ISSN:1860-7179
1860-7187
DOI:10.1002/cmdc.200800172