Synthesis of 4-amidomethyl-1-glucosyl-1,2,3-triazoles and evaluation as glycogen phosphorylase inhibitors.
Carbohydrate Research(2015)
摘要
•Glycogen phosphorylase is a target enzyme for the regulation of glycemia in the context of type 2 diabetes.•Synthesis of 4-amidomethyl-1-glucosyl-1,2,3-triazoles was achieved from the condensation of glucosyl azide and Boc-protected propargyl amine.•Inhibition of GP was in the high micromolar range for the designed inhibitors.•The Boc-carbamate group could be identified as a potential pharmacophore for the inhibition of GP.
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关键词
Carbohydrate,Triazole,Click chemistry,Inhibitor,Glycogen phosphorylase
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