Synthesis and Antipancreatitis Activities of Novel N-(2-Sulfonylamino-5-trifluoromethyl-3-pyridyl)carboxamide Derivatives as Phospholipase A2 Inhibitors.

Abstract

Novel N-(2-sulfonylamino-5-trifluoromethyl-3-pyridyl)carboxamide derivatives have been prepared and evaluated as phospholipase A2 (PLA2) inhibitors. Among these compounds, IS-741 (sodium salt of 1j), which showed the highest and the most stable therapeutic effect on acute hemorrhagic pancreatitis induced by the closed duodenal loop method in rats, was selected as a candidate for further development.