Synthesis and antimalarial activity of novel medium-sized 1,2,4,5-tetraoxacycloalkanes

被引:126
作者
Kim, HS
Nagai, Y
Ono, K
Begum, K
Wataya, Y
Hamada, Y
Tsuchiya, K
Masuyama, A
Nojima, M
McCullough, KJ
机构
[1] Okayama Univ, Fac Pharmaceut Sci, Okayama 7008530, Japan
[2] Osaka Univ, Fac Engn, Dept Chem Mat, Suita, Osaka 5650871, Japan
[3] Heriot Watt Univ, Dept Chem, Edinburgh EH14 4AS, Midlothian, Scotland
关键词
D O I
10.1021/jm010026g
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
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.
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页码:2357 / 2361
页数:5
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