Hydroxyl-substituted sulfonylureas as potent inhibitors of specific [3 H] glyburide binding to rat brain synaptosomes

RA Hill, S Rudra, B Peng, DS Roane, JK Bounds…

Index: Hill, Ronald A.; Rudra, Sonali; Peng, Bo; Roane, David S.; Bounds, Jeffrey K.; Zhang, Yang; Adloo, Ahmad; Lu, Tiansheng Bioorganic and Medicinal Chemistry, 2003 , vol. 11, # 9 p. 2099 - 2113

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Citation Number: 29

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 ...