Discovery of isoxazole voltage gated sodium channel blockers for treatment of chronic pain

A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na v1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-09, Vol.19 (18), p.5334-5338
Hauptverfasser:	Shao, Pengcheng P., Ye, Feng, Weber, Ann E., Li, Xiaohua, Lyons, Kathryn A., Parsons, William H., Garcia, Maria L., Priest, Birgit T., Smith, McHardy M., Felix, John P., Williams, Brande S., Kaczorowski, Gregory J., McGowan, Erin, Abbadie, Catherine, Martin, William J., McMasters, Daniel R., Gao, Ying-Duo
Format:	Artikel
Sprache:	eng
Schlagworte:	Amide replacement Analgesics Animals Biological and medical sciences Cell Line Chronic Disease Heterocycles Humans Inflammatory pain Isoxazole Isoxazoles - chemistry Isoxazoles - pharmacology Isoxazoles - therapeutic use Medical sciences Neuropathic pain Neuropharmacology Pain - drug therapy Pain - immunology Pharmacology. Drug treatments Rats Sodium Channel Blockers - chemistry Sodium Channel Blockers - pharmacology Sodium Channel Blockers - therapeutic use Sodium Channels - metabolism Spinal Nerves - drug effects Structure-Activity Relationship Voltage gated sodium channel blocker
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Zusammenfassung:	A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na v1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement on Na v1.7 inhibitory activity.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.07.135