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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.

journal_name

Bioorg Med Chem Lett

journal_title

Bioorganic & medicinal chemistry letters

authors

Shao PP,Ok D,Fisher MH,Garcia ML,Kaczorowski GJ,Li C,Lyons KA,Martin WJ,Meinke PT,Priest BT,Smith MM,Wyvratt MJ,Ye F,Parsons WH

doi

10.1016/j.bmcl.2005.02.002

subject

Has Abstract

pub_date

2005-04-01 00:00:00

pages

1901-7

issue

7

eissn

0960-894X

issn

1464-3405

pii

S0960-894X(05)00170-8

journal_volume

15

pub_type

杂志文章

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