Add time:07/12/2019         Source:sciencedirect.com

Glycogen phosphorylase (GP) appears as a key enzyme for the control of hyperglycemia in the context of type 2 diabetes. In order to gain additional data for structure–activity studies of the inhibition of this enzyme, a series of eight GP inhibitor candidates were prepared from peracetylglucopyranosyl azide 1 by click-chemistry. The need for a N-Boc-protected propargylamine was identified in the CuAAC with azide 1 under Meldal’s conditions, while Sharpless’ conditions were better adapted to the CuAAC of azide 1 with propargyl bromide. Cycloaddition of Boc-propargylamine with azide 1 afforded the N-Boc precursor of a 4-aminomethyl-1-glucosyl-1,2,3-triazole which gave access to a series of eight amide and sulfonamide derivatives. After deacetylation, enzymatic studies revealed poor to moderate inhibitions toward this enzyme. The N-Boc-protected amine was the best inhibitor (IC50 = 620 μM) unexpectedly slightly better than the 2-naphthylamido substituted analogue (IC50 = 650 μM).

We also recommend Trading Suppliers and Manufacturers of 4-(N-Boc-aminomethyl)-2-Bromopyridine (cas 1049025-21-9). Pls Click Website Link as below: cas 1049025-21-9 suppliers