AI Article Synopsis
- N-(6-Substituted-1,3-benzothiazol-2-yl)benzenesulfonamide derivatives were synthesized and evaluated for their antidiabetic effects in a rat model of non-insulin-dependent diabetes mellitus.
- Several of the synthesized compounds significantly reduced plasma glucose levels.
- The most effective compounds (3 and 4) were docked into the 11beta-HSD1 enzyme structure, suggesting potential hydrogen bond interactions with key active site residues.
Article 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.
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| http://dx.doi.org/10.1016/j.bmcl.2008.03.086 | DOI Listing |
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