| Title | Antidiabetic activity of N-(6-substituted-1,3-benzothiazol-2-yl)benzenesulfonamides. |
| Publication Type | Journal Article |
| Year of Publication | 2008 |
| Authors | Moreno-D{\'ıaz H, Villalobos-Molina R, Ortiz-Andrade R, D{\'ıaz-Coutiño D, Medina-Franco JL, Webster SP, Binnie M, Estrada-Soto S, Ibarra-Barajas M, León-Rivera I, Navarrete-Vázquez G |
| Journal | Bioorganic & medicinal chemistry letters |
| Volume | 18 |
| Pagination | 2871-7 |
| Date Published | 2008 May 1 |
| 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 11beta-hydroxysteroid dehydrogenase type 1 (11beta-HSD1) inhibitors. The most active compounds (3 and 4) were docked into the crystal structure of 11beta-HSD1. Docking results indicate potential hydrogen bond interactions with catalytic amino acid residues. |
