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ID: ALA1138981
Journal: Bioorg Med Chem Lett
Title: Synthesis and SAR of 1,2-trans-(1-hydroxy-3-phenylprop-1-yl)cyclopentane carboxamide derivatives, a new class of sodium channel blockers.
Authors: Ok D, Li C, Abbadie C, Felix JP, Fisher MH, Garcia ML, Kaczorowski GJ, Lyons KA, Martin WJ, Priest BT, Smith MM, Williams BS, Wyvratt MJ, Parsons WH.
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.
CiteXplore: 16337121