Substituted biaryl oxazoles, imidazoles, and thiazoles as sodium channel blockers

A series of low molecular weight biaryl substituted oxazoles, imidazoles, and thiazoles were identified as Na v1.7 blockers. These state dependent sodium channel blockers were synthesized and evaluated for treatment of neuropathic pain. Voltage-gated sodium channels have been shown to play a critica...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2010-09, Vol.20 (18), p.5536-5540
Hauptverfasser:	Tyagarajan, Sriram, Chakravarty, Prasun K., Zhou, Bishan, Fisher, Michael H., Wyvratt, Mathew J., Lyons, Kathy, Klatt, Tracy, Li, Xiaohua, Kumar, Sanjeev, Williams, Brande, Felix, John, Priest, Birgit T., Brochu, Richard M., Warren, Vivien, Smith, McHardy, Garcia, Maria, Kaczorowski, Gregory J., Martin, William J., Abbadie, Catherine, McGowan, Erin, Jochnowitz, Nina, Parsons, William H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Analgesics Animals Biaryl imidazoles Biaryl oxazoles Biaryl thiazoles Biological and medical sciences Dogs Humans Imidazoles - chemistry Imidazoles - metabolism Imidazoles - pharmacology Imidazoles - therapeutic use Medical sciences Microsomes, Liver - metabolism Na v1.7 blockers NAV1.7 Voltage-Gated Sodium Channel Neuralgia - drug therapy Neuropathic pain Neuropathy Neuropharmacology Oxazoles - chemistry Oxazoles - metabolism Oxazoles - pharmacology Oxazoles - therapeutic use Pharmacology. Drug treatments Rats Sodium Channel Blockers - chemistry Sodium Channel Blockers - metabolism Sodium Channel Blockers - pharmacology Sodium Channel Blockers - therapeutic use Sodium Channels - metabolism Thiazoles - chemistry Thiazoles - metabolism Thiazoles - pharmacology Thiazoles - therapeutic use Voltage-gated sodium channel
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