2,4(5)-Diarylimidazoles: synthesis and biological evaluation of a new class of sodium channel blockers against hNa(v)1.2

Bioorg Med Chem Lett. 2008 Oct 15;18(20):5460-2. doi: 10.1016/j.bmcl.2008.09.036. Epub 2008 Sep 11.

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

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Chemistry, Pharmaceutical / methods*
  • Drug Design
  • Humans
  • Imidazoles / chemical synthesis*
  • Imidazoles / pharmacology
  • Ion Channel Gating
  • Models, Chemical
  • Molecular Structure
  • NAV1.2 Voltage-Gated Sodium Channel
  • Nerve Tissue Proteins / antagonists & inhibitors*
  • Nerve Tissue Proteins / chemistry*
  • Protein Isoforms
  • Sodium / chemistry
  • Sodium Channel Blockers / chemical synthesis*
  • Sodium Channel Blockers / chemistry
  • Sodium Channel Blockers / pharmacology
  • Sodium Channels / chemistry*
  • Structure-Activity Relationship

Substances

  • Imidazoles
  • NAV1.2 Voltage-Gated Sodium Channel
  • Nerve Tissue Proteins
  • Protein Isoforms
  • SCN2A protein, human
  • Sodium Channel Blockers
  • Sodium Channels
  • Sodium