Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 44, Issue 4, Pages 1457-1462Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2008.09.044
Keywords
Antimalarial activity; Chlorovinyl sulfones; Chalcones; Synthesis
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Funding
- Consejo de Desarrollo Cientifico y Humanistico (CDCH), Universidad Central de Venezuela [PG 0630-5126, PG 0630-5125-2.003]
- CICNAT, UPEL-IPC [04/070]
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The synthesis of novel chlorovinyl sulfone-like chalcone derivatives and their antimalarial activity against cultured Plasmodium falciparum parasites, hemozoin formation, hemoglobin hydrolysis and murine malaria model are described. Compounds were prepared via Claisen-Schmidt condensation from available chloromethylphenyl sulfones with substituted aldehydes. Antiplasmodial IC50 activity of these compounds ranged between 0.025 and 10 mu M, those that blocked P. falciparum development at low micro molar concentrations were tested in a murine Plasmodium berghei model, and these compounds delayed the progression of malaria but did not eradicate infections. Much effort and attention are needed for discovery and development of new and less toxic antimalarial drugs. (C) 2008 Elsevier Masson SAS. All rights reserved.
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