Pharmacology of the hypoglycaemic sulphonylurea gliquidone. III. Conformational analysis

Pharmacological Research : the Official Journal of the Italian Pharmacological Society
L LinsWilly J Malaisse

Abstract

The hypoglycaemic sulphonylurea gliquidone was found, by conformation analysis, to display a U-shaped configuration, with hydrophobic cycles placed at the extremity of each branch and a peptidic bond placed at the bottom of the U. This configuration is similar to that recently observed with the hypoglycaemic sulphonylureas glimepiride and glibenclamide and non-sulphonylurea hypoglycaemic agents of the meglitinide family, such as S3075, repaglinide, A-4166 and KAD-1229. The identification of a conformation common to these various hypoglycaemic drugs may provide an imprint of their binding site at the level of the B-cell sulphonylurea receptor.

Citations

Jul 15, 2011·Acta Crystallographica. Section E, Structure Reports Online·Thomas GelbrichUlrich J Griesser
Oct 3, 2013·European Journal of Drug Metabolism and Pharmacokinetics·Fan ZhangXinan Wu
Aug 20, 2010·The Journal of Physical Chemistry. B·Yoganjaneyulu KasettiPrasad V Bharatam

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