Identification, biological activity, and mechanism of the anti-ischemic quinolone analog

Bioorg Med Chem. 2007 Oct 15;15(20):6517-26. doi: 10.1016/j.bmc.2007.07.009. Epub 2007 Jul 26.

Abstract

The quinolone analog SQ-4004 has been identified as a potentially excellent anti-ischemic agent, which exhibited highly potent efficacy in reducing infarct volume size in vivo rat MCAO model (32.1% at 0.01mg/kg) and potent cardioprotective effect at myocardial infarction in vivo model (26.6% at 0.01mg/kg) while it exhibited highly reduced anti-bacterial activity. The mechanistic study revealed that the anti-ischemic activity might exert via an anti-apoptotic pathway, which implies its therapeutic uses against the ischemic cell injuries including ischemic stroke and ischemic heart disease.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Bacterial Agents / chemistry
  • Anti-Bacterial Agents / pharmacology
  • Brain Ischemia / drug therapy
  • Brain Ischemia / pathology*
  • Cell Line, Tumor
  • Cell Survival / drug effects
  • Disease Models, Animal
  • Humans
  • Models, Biological
  • Molecular Structure
  • Myocardial Infarction / drug therapy
  • Myocardial Infarction / pathology
  • Quinolines / chemical synthesis
  • Quinolines / chemistry*
  • Quinolines / pharmacology*
  • Quinolines / therapeutic use
  • Rats
  • Structure-Activity Relationship

Substances

  • Anti-Bacterial Agents
  • Quinolines
  • quinoline