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

被引：127

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

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2001年 / 44卷 / 14期

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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