The synthesis and biological evaluation of a range of novel functionalized benzopyrans as potential potassium channel activators

Bioorg Med Chem Lett. 2008 Feb 1;18(3):1237-40. doi: 10.1016/j.bmcl.2007.11.135. Epub 2007 Dec 23.

Abstract

A range of novel benzopyrans have been synthesised and biologically evaluated for K(ATP) channel activity employing cromakalim 1 as a benchmark K(ATP) channel opener. Although the compounds that were evaluated demonstrated a reduced ability to relax phenylephrine stimulated rat thoracic tissue, we provide evidence that benzopyrans 7a-h may be operating via an alternative mechanism than ATP-sensitive K(+) channel activity.

MeSH terms

  • Animals
  • Antihypertensive Agents / chemical synthesis*
  • Antihypertensive Agents / chemistry
  • Antihypertensive Agents / pharmacology*
  • Aorta, Thoracic / drug effects
  • Benzopyrans / chemical synthesis*
  • Benzopyrans / chemistry
  • Benzopyrans / pharmacology*
  • Combinatorial Chemistry Techniques
  • Cromakalim / chemistry
  • Cromakalim / pharmacology
  • Molecular Structure
  • Muscle Relaxation / drug effects
  • Myocytes, Smooth Muscle / drug effects
  • Potassium Channels / agonists*
  • Rats
  • Structure-Activity Relationship

Substances

  • Antihypertensive Agents
  • Benzopyrans
  • Potassium Channels
  • Cromakalim