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N-Arylmethylaminoquercitols, a new series of effective antidiabetic agents having α-glucosidase inhibition and antioxidant activity.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2015 Jun 15; Vol. 25 (12), pp. 2570-3. Date of Electronic Publication: 2015 Apr 22. - Publication Year :
- 2015
-
Abstract
- A new series of N-arylalkylaminoquercitols were synthesized by reductive amination of aminoquercitol bisacetonide 5 and a variety of aryl aldehydes. The targeted N-substituted aminoquercitols having phenolic moiety (7a-7c) displayed significantly enhanced α-glucosidase inhibition, which is 26-32 times more potent than that of the unmodified aminoquercitol 6. In addition, compounds 7a-7c also retained antioxidant activity with relatively more pronounced potency than their original phenolics. This recent finding suggests an approach to develop effective antidiabetic agents by incorporating antioxidative moiety into aminocyclitol core structure.<br /> (Copyright © 2015 Elsevier Ltd. All rights reserved.)
- Subjects :
- Aldehydes chemistry
Antioxidants chemical synthesis
Antioxidants metabolism
Glycoside Hydrolase Inhibitors chemical synthesis
Glycoside Hydrolase Inhibitors metabolism
Hypoglycemic Agents chemical synthesis
Hypoglycemic Agents metabolism
Inositol chemical synthesis
Inositol chemistry
Inositol metabolism
Protein Binding
Structure-Activity Relationship
alpha-Glucosidases metabolism
Antioxidants chemistry
Glycoside Hydrolase Inhibitors chemistry
Hypoglycemic Agents chemistry
Inositol analogs & derivatives
alpha-Glucosidases chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 25
- Issue :
- 12
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 25959812
- Full Text :
- https://doi.org/10.1016/j.bmcl.2015.04.033