文章基本信息

标题：Glycogen Phosphorylase a Inhibitors with a Phenethylphenylphthalimide Skeleton Derived from Thalidomide-Related α-Glucosidase Inhibitors and Liver X Receptor Antagonists
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作者：Kazunori Motoshima ; Minoru Ishikawa ; Kazuyuki Sugita 等
期刊名称：Biological and Pharmaceutical Bulletin
印刷版ISSN：0918-6158
电子版ISSN：1347-5215
出版年度：2009
卷号：32
期号：9
页码：1618-1620
DOI：10.1248/bpb.32.1618
出版社：The Pharmaceutical Society of Japan
摘要：Novel glycogen phosphorylase a (GPa) inhibitors with a phenethylphenylphthalimide skeleton were prepared based on α-glucosidase inhibitors and liver X receptor (LXR) antagonists derived from thalidomide. Their structure–activity relationships were analyzed. Some of the compounds thus prepared showed potent inhibitory activity against rabbit muscle GPa with more than 10-fold greater efficacy than a typical GPa inhibitor, 1,4-dideoxy-1,4-imino- D -arabinitol.
关键词：glycogen phosphorylase;enzyme inhibitor;phthalimide;structure–activity relationship