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

Abstract	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.
Authors	Pengchang P Shao, Dong Ok, Michael H Fisher, Maria L Garcia, Gregory J Kaczorowski, Chunshi Li, Kathryn A Lyons, William J Martin, Peter T Meinke, Birgit T Priest, McHardy M Smith, Matthew J Wyvratt, Feng Ye, William H Parsons
Journal	Bioorganic & medicinal chemistry letters (Bioorg Med Chem Lett) Vol. 15 Issue 7 Pg. 1901-7 (Apr 01 2005) ISSN: 0960-894X [Print] England
PMID	15780630 (Publication Type: Comparative Study, Journal Article)
Chemical References	Amides Analgesics Biphenyl Compounds Cyclopentanes Sodium Channel Blockers Succinates Sulfonamides cyclopentane dicarboxamide Mexiletine
Topics	Administration, Oral Amides (chemical synthesis, chemistry, pharmacology, therapeutic use) Analgesics (chemical synthesis, pharmacology) Animals Biphenyl Compounds (chemistry) Cyclopentanes (chemical synthesis, pharmacology, therapeutic use) Ion Channel Gating (drug effects) Methylation Mexiletine (pharmacology) Pain (drug therapy) Pain Measurement (drug effects) Rats Sodium Channel Blockers (chemical synthesis, pharmacology, therapeutic use) Structure-Activity Relationship Succinates (chemistry) Sulfonamides (chemistry)

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