Article
Hydroxyl-Substituted Sulfonylureas as Potent Inhibitors of Specific [3H]glyburide Binding to Rat Brain Synaptosomes
Bioorganic & Medicinal Chemistry
(2003)
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.
Keywords
- sulfonylureas,
- inhibitors,
- brain synaptosomes
Disciplines
Publication Date
May 1, 2003
DOI
10.1016/S0968-0896(02)00606-5
Citation Information
Ronald A. Hill, Sonali Rudra, Bo Peng, David S. Roane, et al.. "Hydroxyl-Substituted Sulfonylureas as Potent Inhibitors of Specific [3H]glyburide Binding to Rat Brain Synaptosomes" Bioorganic & Medicinal Chemistry Vol. 11 Iss. 9 (2003) p. 2099 - 2113 ISSN: 0968-0896 Available at: http://works.bepress.com/david-s-roane/2/