Antimalarial activity of thiophenyl- and benzenesulfonyl-dihydroartemisinin
Antimalarial activity of thiophenyl- and benzenesulfonyl-dihydroartemisinin
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DOI：
10.3347/kjp.2005.43.3.123
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发表时间：
2005-09-01
影响因子：
--
通讯作者：
Choi, Han-Kyu
中科院分区：
文献类型：
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作者：
Lee, Seokjoon;Oh, Sangtae;Choi, Han-Kyu
以青蒿素为原料，经三步反应合成了10-苯硫基-和10-苯磺酰基-双氢青蒿素的各非对映异构体，并对抗氯喹和抗氯喹敏感的恶性疟原虫进行了筛选。发现四种测试化合物中的三种是有效的。尤其是10 β-苯磺酰基双氢青蒿素的抗疟活性比青蒿素强。
Each diastereomer of 10-thiophenyl- and 10-benzenesulfonyl-dihydroartemisinin was synthesized from artemisinin in three steps, and screened against chloroquine-resistance and chloroquine-sensitive Plasmodium falciparum. Three of the four tested compounds were found to be effective. Especially, 10 beta-benzenesulfonyl-dihydroartemisinin showed stronger antimalarial activity than artemisinin.