Chemical synthesis and preliminary biological evaluation of C-6-O-methyl-1-deoxynojirimycin as a potent α-glucosidase inhibitor

摘要

AbstractA facile and efficient synthesis of 6-O-methyl-1-deoxynojirimycin 4 from commercially available methyl α-D-glucopyranoside in 10 steps and 25% overall yield was reported. The synthetic strategy was based on the regioselective protection/deprotection at 6-O-position and cyclization as the main reaction steps. Compound 4 was evaluated for its inhibitory effect (IC50) on α-glucosidase using an in vitro assay. It showed improved inhibitory activity compared to 1-deoxynojirimycin and acarbose.

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