2-Alkyl-4-arylimidazoles: structurally novel sodium channel modulators.
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.
Liberatore
Anne-Marie
AM
Ipsen Research Laboratories, Institut Henri Beaufour, 5 avenue du Canada, 91966 Les Ulis, France. anne-marie.liberatore@ipsen.com
Schulz
Jocelyne
J
Pommier
Jacques
J
Barthelemy
Marie-Anne
MA
Huchet
Marion
M
Chabrier
Pierre-Etienne
PE
Bigg
Dennis
D
D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis / Q000494:pharmacology; D001665:Binding Sites; D001921:Brain / Q000378:metabolism; D002243:Carbolines / Q000737:chemistry; D002478:Cells, Cultured; D004594:Electrophysiology; D020128:Inhibitory Concentration 50; D051381:Rats; D026941:Sodium Channel Blockers / Q000138:chemical synthesis* / Q000494:pharmacology; D015222:Sodium Channels / Q000378:metabolism*; D013329:Structure-Activity Relationship; D014701:Veratridine / Q000494:pharmacology
D001562:Benzimidazoles; D002243:Carbolines; D026941:Sodium Channel Blockers; D015222:Sodium Channels; D014701:Veratridine