Pharmacology of the hypoglycaemic sulphonylurea gliquidone. III. Conformational analysis.

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.