Synthesis and blood glucose and lipid-lowering effects of benzothiazole-substituted benzenesulfonylurea derivatives

摘要

Sulfonylurea drugs are widely used for the therapy of non-insulin-dependent diabetes mellitus. These drugs improve glucose and lipid levels by stimulating insulin secretion by the pancreatic beta-cell comprising two generations with the second one more potent than the first. Glibenclamide is a well-known and potent second-generation sulfonylurea oral hypoglycemic drug which is most widely used in type II diabetes. In this research, five new analogs were synthesized by exchanging the lipophilic phenyl and urea moieties in the first and the end of the molecule with chlorobenzamide and hydrophilic and antidiabetic aminobenzothiazole substituents. Their glucose and lipid-lowering activities were evaluated and compared to the standard drug. Results showed that all of the new compounds exhibited better activities. In addition, in particular aminomethylbenzothiazoles derivatives could have exerted prominent hypoglycemic and a noticeable hypolipidemic effects superior to glibenclamide.