Novel five-membered iminocyclitol derivatives as selective and potent glycosidase inhibitors: New structures for antivirals and osteoarthritis

被引:106
作者
Liang, PH
Cheng, WC
Lee, YL
Yu, HP
Wu, YT
Lin, YL
Wong, CH
机构
[1] Acad Sinica, Genom Res Ctr, Taipei 11529, Taiwan
[2] Acad Sinica, Inst Biomed Sci, Taipei 11529, Taiwan
[3] Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
[4] Scripps Res Inst, Skaggs Inst Chem Biol, La Jolla, CA 92037 USA
关键词
antiviral agents; glycoproteins; iminocyclitols; inhibitors; osteoarthritis;
D O I
10.1002/cbic.200500321
中图分类号
Q5 [生物化学]; Q7 [分子生物学];
学科分类号
071010 ; 081704 ;
摘要
A novel 5-membered iminocyclitol derivative was found to be a potent and selective inhibitor of the glycoprotein-processing alpha-glucosidase with a K-i value of 53 nM. This compound was further derivatized to antiviral agents against Japanese encephalitis virus, dengue virus serotype 2 (DEN-2), human SARS coronavirus, and human beta-hexosaminidase (K-i = 2.6 rim), a new target for the development of osteoarthritis therapeutics.
引用
收藏
页码:165 / 173
页数:9
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