Journal
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
Volume 108, Issue -, Pages 134-140Publisher
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.11.020
Keywords
Naphthoquinones; Lapachone; Epoxides; Malaria; Infectious disease
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Funding
- CNPq (National Council of Research of Brazil)
- CAPES
- FAPERJ
- PRONEX FAPERJ [E-26/110.574/2010]
- CNPq [304716/2014-6]
- PRONEX FAPEAM NOSSAPLAM Project [Edital 023/2009]
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A series of eighteen quinones and structurally-related oxiranes were synthesized and evaluated for in vitro inhibitory activity against the chloroquine-sensitive 3D7 clone of the human malaria parasite Plasmodium falciparum. 2-amino and 2-allyloxynaphthoquinones exhibited important antiplasmodial activity (median inhibitory concentrations (IC50) < 10 mu M). Oxiranes 6 and 25, prepared respectively by reaction of alpha-lapachone and tetrachloro-p-quinone with diazomethane in a mixture of ether and ethanol, exhibited the highest antiplasmodial activity and low cytotoxicity against human fibroblasts (MCR-5 cell line). The active compounds could represent a good prototype for an antimalarial lead molecule. (C) 2015 Published by Elsevier Masson SAS.
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