Bian X, et al. (2013) A new series of N2-substituted-5-(p-toluenesulfonylamino)phthalimide analogues as a-glucosidase inhibitors. Bioorg Med Chem Lett 23(7):2022-6
Abstract: Several members of a new family of non-sugar-type a-glycosidase inhibitors, bearing a 5-(p-toluenesulfonylamino)phthalimide moiety and various substituent at the N2 position, were synthesized and their activities were investigated. The newly synthesized compounds displayed different inhibition profile towards yeast a-glycosidase and rat intestinal a-glycosidase. Almost all the compounds had strong inhibitory activities against yeast a-glycosidase. Regarding rat intestinal a-glycosidase, only analogs with N2-aromatic substituents displayed varying degrees of inhibitory activities on rat intestinal maltase and lactase and nearly all compounds showed no inhibition against rat intestinal a-amylase. Structure-activity relationship studies indicated that 5-(p-toluenesulfonylamino)phthalimide moiety is a favorable scaffold to exert the a-glucosidase inhibitory activity and substituents at the N2 position have considerable influence on the efficacy of the inhibition activities.
|Status: Published||Type: Journal Article | Research Support, Non-U.S. Gov't||PubMed ID: 23466232|