Abstract
A small family of novel 2,4(5)-diarylimidazoles were prepared through a simple and efficient synthesis and evaluated as potential inhibitors of hNa(v)1.2 sodium channel currents. One member of this series (4) exhibited profound inhibition of Na(v)1.2 currents, emerging as a promising lead compound for further structure-activity relationship studies for the development of novel sodium channel blockers.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Chemistry, Pharmaceutical / methods*
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Drug Design
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Humans
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology
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Ion Channel Gating
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Models, Chemical
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Molecular Structure
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NAV1.2 Voltage-Gated Sodium Channel
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Nerve Tissue Proteins / antagonists & inhibitors*
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Nerve Tissue Proteins / chemistry*
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Protein Isoforms
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Sodium / chemistry
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Sodium Channel Blockers / chemical synthesis*
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Sodium Channel Blockers / chemistry
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Sodium Channel Blockers / pharmacology
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Sodium Channels / chemistry*
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Structure-Activity Relationship
Substances
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Imidazoles
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NAV1.2 Voltage-Gated Sodium Channel
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Nerve Tissue Proteins
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Protein Isoforms
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SCN2A protein, human
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Sodium Channel Blockers
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Sodium Channels
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Sodium