Synthesis and antiviral activity of novel exomethylene cyclopropyl pyrimidine nucleosides

被引:0
|
作者
Kook, MC
Kim, G
Kwak, EY
Hong, JH
Lee, CK
Choi, BG [1 ]
机构
[1] Chonnam Natl Univ, Coll Pharm, Dept Med Chem, Kwangju 500757, South Korea
[2] Chosun Univ, Coll Pharm, Dept Med Chem, Kwangju 501759, South Korea
[3] Korea Res Inst Chem Technol, Pharmaceut Screening Ctr, Taejon 306600, South Korea
关键词
exomethylene cyclopropyl nucleoside; antiviral agent; Feist's acid;
D O I
10.1007/BF02976993
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of novel exomethylene cyclopropyl nucleosides have been synthesized starting from Feist's acid. Classical nucleophilic substitution conditions (K2CO3, 18-crown-6) of the tosylate 2 as well as Mitsunobu reaction (DEAD, PPh3) of alcohol 1 with pyrimidine bases afforded a series of novel cyclopropyl nucleosides. Compound 4b displayed moderate anti-HBV activity without any cytotoxicity up to 100 muM.
引用
收藏
页码:790 / 794
页数:5
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