1.
Bioorg Med Chem Lett
; 17(6): 1746-9, 2007 Mar 15.
Article
in English
| MEDLINE
| ID: mdl-17234409
ABSTRACT
A series of 4-arylimidazole carbamates was synthesized and their binding affinities to the site-2 sodium (Na+) channel were determined. SAR studies led to the identification of compound 10, a potent Na+ channel blocker which was efficacious in pain models in vivo.
Subject(s)
Carbamates/chemical synthesis , Carbamates/pharmacology , Imidazoles/chemical synthesis , Imidazoles/pharmacology , Pain/drug therapy , Pain/etiology , Peripheral Nervous System Diseases/complications , Sodium Channel Blockers/chemical synthesis , Sodium Channel Blockers/pharmacology , Animals , Batrachotoxins , Binding, Competitive/drug effects , Carrageenan , Humans , Hyperalgesia/chemically induced , Hyperalgesia/drug therapy , Indicators and Reagents , Microsomes/drug effects , Microsomes/metabolism , Rats , Sodium/metabolism , Structure-Activity Relationship , Synaptosomes/drug effects , Synaptosomes/metabolism , Veratridine/pharmacology
2.
Bioorg Med Chem Lett
; 14(13): 3521-3, 2004 Jul 05.
Article
in English
| MEDLINE
| ID: mdl-15177465
ABSTRACT
A series of 2-alkyl-4-arylimidazoles were prepared and their binding affinities to the site-2 sodium (Na+) channel were determined. SAR studies led to highly potent Na+ channel blockers.