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. 2006 Mar 1;16(5):1358-61.
doi: 10.1016/j.bmcl.2005.11.051. Epub 2005 Dec 5.

Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers

Dong Ok  1 , Chunshi Li, Catherine Abbadie, John P Felix, Michael H Fisher, Maria L Garcia, Gregory J Kaczorowski, Kathryn A Lyons, William J Martin, Birgit T Priest, McHardy M Smith, Brande S Williams, Matthew J Wyvratt, William H Parsons
Affiliations

Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers

Dong Ok et al. Bioorg Med Chem Lett. .

Abstract

Novel cyclopentane-based 3-phenyl-1-hydroxypropyl compounds were evaluated for inhibitory activity against the peripheral nerve sodium channel Na(V)1.7 and off-target activity against the cardiac potassium channel hERG. The stereochemistry of the hydroxyl group and substitution on the phenyl rings with either fluorinated O-alkyl or alkyl groups were found to be critical for conferring potency against Na(V)1.7. A benchmark compound from this series displayed efficacy in rat models of inflammatory and neuropathic pain.

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