Author/Authors :
Ronald A. Hill، نويسنده , , Sonali Rudra، نويسنده , , Bo Peng، نويسنده , , David S. Roane، نويسنده , , Jeffrey K. Bounds، نويسنده , , Yang Zhang، نويسنده , , Ahmad Adloo، نويسنده , , Tiansheng Lu، نويسنده ,
Abstract :
We are seeking to discover potent CNS-active sulfonylureas with structural features that allow for the formation of several types of prodrugs. We report herein the syntheses of compounds comprising an initial series of hydroxyl-substituted analogues of the potent ATP-sensitive potassium channel blockers glyburide (glibenclamide) and gliquidone. Somewhat unexpectedly, several of the compounds were found to be comparably potent to glyburide as inhibitors of specific [3H]glyburide binding in rat brain preparations.