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.
Lins
L
L
Centre de Biophysique Moléculaire Numérique, Faculté Universitaire de Gembloux, Belgium.
Brasseur
R
R
Malaisse
W J
WJ
D007004:Hypoglycemic Agents / Q000737:chemistry* / Q000494:pharmacology*; D008968:Molecular Conformation; D013329:Structure-Activity Relationship; D013453:Sulfonylurea Compounds / Q000737:chemistry* / Q000494:pharmacology*
D007004:Hypoglycemic Agents; D013453:Sulfonylurea Compounds; C010969:gliquidone