Synthesis and antiplasmodial activity of lycorine derivatives
Synthesis and antiplasmodial activity of lycorine derivatives
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DOI：
10.1016/j.bmc.2010.05.023
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发表时间：
2010-07-01
影响因子：
3.5
通讯作者：
Estevez-Braun, Ana
中科院分区：
文献类型：
--
作者：
Cedron, Juan C.;Gutierrez, David;Estevez-Braun, Ana
制备了27个石蒜碱衍生物，并对其体外抗恶性疟原虫氯喹敏感株的活性进行了评价。当石蒜碱衍生物在C-1和C-2上呈现自由羟基或以乙酸酯或异丁酸酯的形式酯化时，其抗疟原虫活性最好。双键C-2-C-3对活性也很重要。在抗疟原虫活性方面，亚甲二氧基被羟基或乙酸基取代，甲基取代基接在氮原子上，得到较高的抗原虫活性。(C)2010爱思唯尔有限公司。保留所有权利。
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.