3-Alkylamino-pyrido[4,3-<I>e</I>]-1,2,4-thiadiazine 1,1-dioxides as Potent K<SUB>ATP</SUB>-Channel Activators: Structural Study and Influence of Stereochemistry

Abstract

Pyrido[4,3‐e]‐1,2,4‐thiadiazine 1,1‐dioxides bearing a short and branched alkylamino side chain in the 3 position, appear to be powerful and tissue selective pancreatic KATP‐channel activators. In order to confirm the pharmacophoric model for the activation of pancreatic KATP channels, a structural study was undertaken on representative 3‐alkyl‐aminopyridothiadiazines. The influence on the biological activity of the stereochemistry associated to the first carbon atom of the 3‐alkylamino chain was also examined.