Synthesis of new 6-alkylvinyl/arylalkylvinyl substituted 1,2,4-trioxanes active against multidrug-resistant malaria in mice
- 作者：Singh ; Chandan ; Gupta ; Nitin ; Puri ; Sunil K.
- 关键词：Artemisinin ; Antimalarial ; 1 ; 2 ; 4-Trioxane ; Photooxygenation ; Plasmodium yoelii
- 刊名：Bioorganic and Medicinal Chemistry
- 出版年：2004
- 期刊代码：9_09680896
- 类别：ch
- 出版时间：November 1, 2004
- 卷：12
- 期：21
- 页码：5553-5562
- 文件大小：327 K
摘要
3-Alkyl/arylalkyl substituted 2-butenols 9, 10, 23a芒芒芒d undergo regiospecific photooxygenation to furnish 芒芒-hydroxyhydroperoxides 11, 12, 24a芒芒芒d, respectively, in reasonable yields. Acid catalyzed condensation of 11, 12, 24a芒芒芒d with various ketones furnish new 1,2,4-trioxanes 13芒芒芒18, 25a芒芒芒d, 26a芒芒芒d, 27a芒芒芒d in good yields. Several of these trioxanes show promising antimalarial activity against multidrug-resistant Plasmodium yoelii in mice by oral and intramuscular routes.