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

页码：1494 / 1499

页数：6

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