Synthesis and Biological Evaluation of Sulfonylcyanoguanidines and Sulfonamidonitroethylenes as Bioisosteres of Hypoglycemic Sulfonylureas.

Summary Sulfonylcyanoguanidines and sulfonamidonitroethylenes are bioisosteres of hypoglycemic sulfonylureas and were prepared and evaluated for their insulin release potency from rat pancreatic islets. At 25 μM, both bioisosteres of glibenclamide, sulfonylcyanoguanidine 22 and sulfonamidonitroethylene 23 , were as potent as their parent on insulin secretion.