ACID DEGRADATION PRODUCTS OF QINGHAOSU AND THEIR STRUCTURE-ACTIVITY-RELATIONSHIPS
ACID DEGRADATION PRODUCTS OF QINGHAOSU AND THEIR STRUCTURE-ACTIVITY-RELATIONSHIPS
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DOI：
10.3987/com-90-5396
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发表时间：
1990-06-01
期刊：
影响因子：
0.6
通讯作者：
LEE, KH
中科院分区：
文献类型：
--
作者：
IMAKURA, Y;HACHIYA, K;LEE, KH
青蒿素（1）经酸处理后，生成1“，2”，4“-三恶烷（5和8）、内过氧化物（6和9）和二酮（7和10）。5、6、7、8、9和10的结构基于它们的物理和光谱数据被指定。这些化合物的构效关系表明，1“，2”，4“-三恶烷环系统的空间位阻要求是有效的抗疟活性。
Treatment of qinghaosu (1) with acid yielded 1'',2'',4''-trioxanes (5 and 8), endoperoxides (6 and 9), and diketones (7 and 10). Structures of 5, 6, 7, 8, 9, and 10 were assigned based on their physical and spectral data. Structure-activity correlation among these compounds indicated the steric requirement of the 1'',2'',4''-trioxane ring system as found in 1 for ptoent antimalarial activity.