Novel α-glucosidase inhibitors with a tetrachlorophthalimide skeleton
| Autor: | Hiroyasu Takahashi, Mikiko Sodeoka, Ryu Yamasaki, Satoshi Mayumi, Shizuo Kadoya, Yuichi Hashimoto, Sonei Sou |
|---|---|
| Rok vydání: | 2000 |
| Předmět: |
1-Deoxynojirimycin
Binding Sites Stereochemistry Chemistry α glucosidase Organic Chemistry Clinical Biochemistry Pharmaceutical Science Phthalimides alpha-Glucosidases Biochemistry Skeleton (computer programming) Inhibitory Concentration 50 Structure-Activity Relationship Catalytic Domain Drug Discovery Molecular Medicine Glycoside Hydrolase Inhibitors Enzyme Inhibitors Molecular Biology |
| Zdroj: | Bioorganic & Medicinal Chemistry Letters. 10:1081-1084 |
| ISSN: | 0960-894X |
| DOI: | 10.1016/s0960-894x(00)00161-x |
| Popis: | Novel alpha-glucosidase inhibitors with a tetrachlorophthalimide skeleton were prepared and their structure-activity relationships were analyzed. Among them, N-phenyl-4,5,6,7-tetrachlorophthalimide (CPOP: 2) and N-(4-phenylbutyl)-4,5,6,7-tetrachlorophthalimide (CP4P: 6) showed very potent inhibitory activity, being more potent than 1-deoxynojirimycin (dNM: 1). Mechanistic studies revealed that CPOP (2) and CP4P (6) inhibit alpha-glucosidase non-competitively and competitively, respectively. |
| Databáze: | OpenAIRE |
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