Author/Authors :
Hermenegilda Moreno-Diaz، نويسنده , , Rafael Villalobos-Molina، نويسنده , , Rolffy Ortiz-Andrade، نويسنده , , Daniel D?az-Couti?o، نويسنده , , José Luis Medina-Franco، نويسنده , , Scott P. Webster، نويسنده , , Margaret Binnie، نويسنده , , Samuel Estrada-Soto، نويسنده , , Maximiliano Ibarra-Barajas، نويسنده , , Ismael Le?n-Rivera، نويسنده , , Gabriel Navarrete-V?zquez، نويسنده ,
Abstract :
N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives 1–8 were synthesized and evaluated for their in vivo antidiabetic activity in a non-insulin-dependent diabetes mellitus rat model. Several compounds synthesized showed significant lowering of plasma glucose level in this model. As a possible mode of action, the compounds were in vitro evaluated as 11β-hydroxysteroid dehydrogenase type 1 (11β-HSD1) inhibitors. The most active compounds (3 and 4) were docked into the crystal structure of 11β-HSD1. Docking results indicate potential hydrogen bond interactions with catalytic amino acid residues.
