Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 19, Issue 18, Pages 5334-5338Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2009.07.135
Keywords
Voltage gated sodium channel blocker; Neuropathic pain; Inflammatory pain; Amide replacement; Heterocycles; Isoxazole
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A series of novel isoxazole voltage gated sodium channel blockers have been synthesized and evaluated. Substitutions on the benzylic position of benzamide were investigated to determine their effect on Na(v)1.7 inhibitory potency. The spirocyclobutyl substitution had the most significant enhancement on Na(v)1.7 inhibitory activity. (C) 2009 Elsevier Ltd. All rights reserved.
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