Novel cyclopentane dicarboxamide sodium channel blockers as a potential treatment for chronic pain

[Display omitted] A series of new voltage-gated sodium channel blockers were prepared based on the screening lead succinic diamide BPBTS. Replacement of the succinimide linker with the more rigid cyclic 1,2- trans-diamide linker was well tolerated. N-Methylation on the biphenylsulfonamide side of th...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2005-04, Vol.15 (7), p.1901-1907
Hauptverfasser:	Shao, Pengchang P., Ok, Dong, Fisher, Michael H., Garcia, Maria L., Kaczorowski, Gregory J., Li, Chunshi, Lyons, Kathryn A., Martin, William J., Meinke, Peter T., Priest, Birgit T., Smith, McHardy M., Wyvratt, Matthew J., Ye, Feng, Parsons, William H.
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Amides - chemical synthesis Amides - chemistry Amides - pharmacology Amides - therapeutic use Analgesics Analgesics - chemical synthesis Analgesics - pharmacology Animals Biological and medical sciences Biphenyl Compounds - chemistry Chronic pain Cyclopentanes - chemical synthesis Cyclopentanes - pharmacology Cyclopentanes - therapeutic use Ion Channel Gating - drug effects Medical sciences Methylation Mexiletine - pharmacology Neuropathic pain Neuropharmacology Pain - drug therapy Pain Measurement - drug effects Pharmacology. Drug treatments Rats Sodium channel blocker Sodium Channel Blockers - chemical synthesis Sodium Channel Blockers - pharmacology Sodium Channel Blockers - therapeutic use Structure-Activity Relationship Succinates - chemistry Sulfonamides - chemistry
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Zusammenfassung:	[Display omitted] A series of new voltage-gated sodium channel blockers were prepared based on the screening lead succinic diamide BPBTS. Replacement of the succinimide linker with the more rigid cyclic 1,2- trans-diamide linker was well tolerated. N-Methylation on the biphenylsulfonamide side of the amide moiety significantly reduced the clearance rate in rat pharmacokinetic studies.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2005.02.002