Synthesis of 2-fluoronoraristeromycin and its inhibitory activity against Plasmodium falciparum S-adenosyl-L-homocysteine hydrolase

被引:39
|
作者
Kitade, Y
Kojima, H
Zulfiqur, F
Kim, HS
Wataya, Y
机构
[1] Gifu Univ, Fac Engn, Dept Biomol Sci, Gifu 5011193, Japan
[2] Okayama Univ, Fac Pharmaceut Sci, Okayama 7008530, Japan
关键词
D O I
10.1016/j.bmcl.2003.08.074
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Palladium-coupling reaction of (IS, 4 R)-cis-4-acetoxy-2-cyclopenten-1-ol with sodium salt of 2-fluoroadenine resulted in the formation of (IS,4R)-4-(6-amino-2-fluoro-9H-purin-9-yl)cyclopent-2-en-1-ol. Subsequent oxidation was carried out with osmium tetraoxide (OsO4) in the presence of 4-methylmorpholine N-oxide (NMO) to give 2-fluoronoraristeromycin, possessing significant inhibitory activity against recombinant Plasm odium falciparum SAH hydrolase. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:3963 / 3965
页数:3
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