Rapid diversity-oriented synthesis in microtiter plates for in situ screening:: Discovery of potent and selective α-fucosidase inhibitors

被引:118
作者
Wu, CY
Chang, CF
Chen, JSY
Wong, CH
Lin, CH
机构
[1] Acad Sinica, Inst Biol Chem, Taipei 11529, Taiwan
[2] Acad Sinica, Ctr Gene Res, 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
D O I
10.1002/anie.200351823
中图分类号
O6 [化学];
学科分类号
0703 ;
摘要
An efficient and simple method has been developed to identify potent and selective inhibitors against α-fucosidases based on the amide-forming reaction in a microtiter plate of a fuconojirimycin core with various carboxylic acids, followed by a direct inhibition assay without product isolation. The structures of the two most potent inhibitors are shown.
引用
收藏
页码:4661 / 4664
页数:4
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