Synthesis and antimalarial activity of novel medium-sized 1,2,4,5-tetraoxacycloalkanes
Synthesis and antimalarial activity of novel medium-sized 1,2,4,5-tetraoxacycloalkanes
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DOI：
10.1021/jm010026g
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发表时间：
2001-07-05
影响因子：
7.3
通讯作者：
McCullough, KJ
中科院分区：
文献类型：
--
作者：
Kim, HS;Nagai, Y;McCullough, KJ
CsOH-或Ag 2 O-介导的（亚烷基）双过氧化物3和1的环烷基化，n.-二卤代烷烃（n = 3-8）以中等产率提供相应的中等大小的1，2，4，5-四氧杂环烷烃4-8。随后对环过氧化物4-8的体外和体内抗疟活性的评价表明，1，2，6，7-四氧杂螺[7.11]十九烷4a作为一种新的、廉价的和有效的抗疟药物具有相当大的潜力。
CsOH- or Ag2O-mediated cycloalkylation of (alkylidene)bisperoxides 3 and 1,n.-dihaloalkanes (n = 3-8) provided the corresponding medium-sized 1,2,4,5-tetraoxacycloalkanes 4-8 in moderate yields. Subsequent evaluation of the antimalarial activity of the cyclic peroxides 4-8 in vitro and in vivo revealed that 1,2,6,7-tetraoxaspiro [7.11]nonadecane 4a has considerable potential as a new, inexpensive, and potent antimalarial drug.