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

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 bloc...

Ausführliche Beschreibung

Gespeichert in:

Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry 2003-05, Vol.11 (9), p.2099-2113
Hauptverfasser:	Hill, Ronald A., Rudra, Sonali, Peng, Bo, Roane, David S., Bounds, Jeffrey K., Zhang, Yang, Adloo, Ahmad, Lu, Tiansheng
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Brain - drug effects Brain - metabolism Dose-Response Relationship, Drug General and cellular metabolism. Vitamins Glyburide - antagonists & inhibitors Glyburide - metabolism Hydroxides - chemistry Hydroxides - pharmacology Medical sciences Pharmacology. Drug treatments Protein Binding - drug effects Protein Binding - physiology Rats Sulfonylurea Compounds - chemistry Sulfonylurea Compounds - pharmacology Synaptosomes - drug effects Synaptosomes - metabolism Tritium - metabolism
Online-Zugang:	Volltext
Tags:	Tag hinzufügen Keine Tags, Fügen Sie den ersten Tag hinzu!

Beschreibung
Zusammenfassung:	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. Graphic
ISSN:	0968-0896 1464-3391
DOI:	10.1016/S0968-0896(02)00606-5