Abstract
Analogs of the previously reported voltage gated sodium channel blocker CDA54 were prepared in which one of the amide functions was replaced with aromatic and non-aromatic heterocycles. Replacement of the amide with an aromatic heterocycle resulted in significant loss of sodium channel blocking activity, while non-aromatic heterocycle replacements were well tolerated.
MeSH terms
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Animals
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Isoxazoles / chemistry*
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Isoxazoles / pharmacology*
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Isoxazoles / therapeutic use
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Models, Molecular
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Molecular Structure
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Pain / drug therapy
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Rats
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Rats, Sprague-Dawley
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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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Spinal Nerves / drug effects
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Structure-Activity Relationship
Substances
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Isoxazoles
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Sodium Channel Blockers