期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 18, 期 13, 页码 4694-4701出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2010.05.023
关键词
Alkaloids; Amaryllidaceae; Lycorine; Plasmodium falciparum
资金
- Spanish MEC [SAF 2006-06720, SAF 2009-13296-C02-01]
- ICIC (Instituto Canario de Investigacion del Cancer)
- Gobierno Autonomo de Canarias
Twenty seven lycorine derivatives were prepared and evaluated for their in vitro antimalarial activity against chloroquine-sensitive strains of Plasmodium falciparum. The best antiplasmodial activities were achieved with lycorine derivatives that present free hydroxyl groups at C-1 and C-2 or esterified as acetates or isobutyrates. The double bond C-2-C-3 is also important for the activity. Concerning to the antiplasmodial activity of the secolycorines, the higher values were obtained with the replacement of the methylenedioxy moiety by hydroxyl or acetate groups and with methyl substituent attached to the nitrogen atom. (C) 2010 Elsevier Ltd. All rights reserved.
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