AI Article Synopsis
- The enzyme α-glucosidase is important for carbohydrate digestion, cell functions, tumor development, and viral infections, leading to interest in its inhibitors.
- A new class of azasugars with various N-substituents was created and tested for their ability to inhibit α-glucosidase, revealing key structural effects on their efficacy.
- The compound N-heteroarylmethyl-5-hydroxy-1,2,5,6-tetrahydropyridine-3-carboxylic acid was identified as a strong inhibitor, using a unique reversible uncompetitive mechanism, showing potential for drug development unlike existing inhibitors like Acarbose.
Article Abstract
The enzyme α-glucosidase has attracted interest owing to its involvement in the digestive process of carbohydrate, its role in intracellular glycoprotein trafficking, tumorigenesis and viral infection. In this study, several members of a new family of N-heteroarylmethyl substituted azasugars were synthesized and evaluated as α-glucosidase inhibitors. We systematically investigated the effect of different N-substituents as well as the role of hydroxyl and carboxylate moieties on the piperidine ring. The compounds N-heteroarylmethyl-5-hydroxy-1,2,5,6-tetrahydropyridine-3-carboxylic acid emerged as potent α-glucosidase inhibitors. Unlike Acarbose and other clinically relevant α-glucosidase inhibitors, these compounds act through a reversible uncompetitive mechanism of inhibition which make them attractive candidates for drug development.
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| http://dx.doi.org/10.1016/j.bmc.2013.07.012 | DOI Listing |
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