Abstract
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.
MeSH terms
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Animals
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Cell Line
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Chronic Disease
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Humans
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Isoxazoles / chemistry
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Isoxazoles / pharmacology
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Isoxazoles / therapeutic use*
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Pain / drug therapy*
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Pain / immunology
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Rats
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Sodium Channel Blockers / chemistry
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Sodium Channel Blockers / pharmacology
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Sodium Channel Blockers / therapeutic use*
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Sodium Channels / metabolism*
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Spinal Nerves / drug effects
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Structure-Activity Relationship
Substances
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Isoxazoles
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Sodium Channel Blockers
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Sodium Channels