α-glucosidase inhibitors with a phthalimide skeleton:: Structure-activity relationship study

被引：0
|
作者：
Takahashi, H [1 ]
Sou, S [1 ]
Yamasaki, R [1 ]
Sodeoka, M [1 ]
Hashimoto, Y [1 ]
机构：
[1] Univ Tokyo, Inst Mol & Cellular Biosci, Bunkyo Ku, Tokyo 1130032, Japan
来源：
CHEMICAL & PHARMACEUTICAL BULLETIN | 2000年 / 48卷 / 10期
关键词：
alpha-glucosidase; enzyme inhibitor; phthalimide; tetrachlorophthalimide; structure-activity relationship;
D O I：
暂无
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
alpha-Glucosidase inhibitors with a phthalimide skeleton were prepared. Structure-activity relationship studies indicated a critical role for the hydrophobicity of the substituent at the nitrogen atom of the phthalimide skeleton. Introduction of electron-withdrawing groups, including a nitro group and chlorine, influenced the activity. Optimization studies led us to design 4,5,6,7-tetrachluro-N-phenylphthalimide (CPOP) and its N-phenylalkyl derivatives. CPOP and 4.5,6,7-tetrachloro-N-(4-phenylbutyl)phthalimide (CP4P) proved to be more potent alpha-glucosidase inhibitors than the known inhibitor 1-deoxynojirimycin.
引用
收藏
页码：1494 / 1499
页数：6
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