Synthesis and antiplasmodial activity of lycorine derivatives

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• 作者：Juan C. Cedró ; n ; David Gutié ; rrez ; Ninoska Flores ; Á ; ngel G. Ravelo ; Ana Esté ; vez-Braun
• 关键词：Alkaloids ; Amaryllidaceae ; Lycorine ; Plasmodium falciparum
• 刊名：Bioorganic and Medicinal Chemistry
• 出版年：2010
• 出版时间：1 July 2010
• 年：2010
• 卷：18
• 期：13
• 页码：4694-4701
• 全文大小：302 K

文摘

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.