51. Flavones as isosteres of 4(1H)-quinolones: discovery of ligand efficient and dual stage antimalarial lead compounds.
- Author
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Rodrigues T, Ressurreição AS, da Cruz FP, Albuquerque IS, Gut J, Carrasco MP, Gonçalves D, Guedes RC, dos Santos DJ, Mota MM, Rosenthal PJ, Moreira R, Prudêncio M, and Lopes F
- Subjects
- Antimalarials chemical synthesis, Antimalarials chemistry, Dose-Response Relationship, Drug, Flavones chemical synthesis, Flavones chemistry, Ligands, Models, Molecular, Molecular Structure, Parasitic Sensitivity Tests, Structure-Activity Relationship, Antimalarials pharmacology, Flavones pharmacology, Plasmodium berghei drug effects, Plasmodium falciparum drug effects, Quinolones chemistry
- Abstract
Malaria is responsible for nearly one million deaths annually, and the increasing prevalence of multi-resistant strains of Plasmodium falciparum poses a great challenge to controlling the disease. A diverse set of flavones, isosteric to 4(1H)-quinolones, were prepared and profiled for their antiplasmodial activity against the blood stage of P. falciparum W2 strain, and the liver stage of the rodent parasite Plasmodium berghei. Ligand efficient leads were identified as dual stage antimalarials, suggesting that scaffold optimization may afford potent antiplasmodial compounds., (Copyright © 2013 Elsevier Masson SAS. All rights reserved.)
- Published
- 2013
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