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

…, D Ok, MH Fisher, ML Garcia, GJ Kaczorowski…

文献索引：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. Bioorganic and Medicinal Chemistry Letters, 2005 , vol. 15, # 7 p. 1901 - 1907

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被引用次数: 23

摘要

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.