Conversion of antimalarial drug artemisinin to a new series of tricyclic 1,2,4-trioxanes

被引:15
作者
Singh, Chandan [1 ]
Chaudhary, Sandeep [1 ]
Kanchan, Rani [1 ]
Puri, Sunil K. [1 ]
机构
[1] Cent Drug Res Inst, Div Med & Proc Chem, Div Parasitol, Lucknow 226001, Uttar Pradesh, India
关键词
D O I
10.1021/ol701887x
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A highly efficient route for the conversion of the antimalarial drug artemisinin to a novel hydroxy-functionalized tricyclic 1,2,4-triaxane 6 is reported. Neither the trioxane 6 nor its derivatives 14-16, all of which lack the hydrolytically unstable acetal-lactone linkage, show antimalarial activity comparable with that of artemisinin.
引用
收藏
页码:4327 / 4329
页数:3
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