Synthesis and cardiac effects of 3,4-dihydropyrimidin-2(1H)-one-5 carboxylates

Bioorg Med Chem Lett. 2006 Sep 15;16(18):4893-7. doi: 10.1016/j.bmcl.2006.06.059. Epub 2006 Jul 7.

Abstract

A series of 4-(substituted)-3,4-dihydropyrimidinone derivatives have been synthesized by heating 1,3 dicarbonyl compounds, urea, and aromatic aldehydes in acetic acid under microwave irradiation conditions. The cardiovascular effects of 3,4-dihydropyrimidinones were studied on isolated perfused frog heart at different dose levels and compared with the activity of digoxin. The interaction of 3,4-dihydropyrimidinones with beta-blocker and calcium channel blocker was also investigated. Compound 4d emerged as the most interesting compound in this series with potential cardiotonic activity.

MeSH terms

  • Animals
  • Anura
  • Carboxylic Acids / chemical synthesis
  • Carboxylic Acids / chemistry*
  • Carboxylic Acids / pharmacology*
  • Heart / drug effects*
  • Heart Rate / drug effects
  • Hydrogen / chemistry*
  • Molecular Structure
  • Pyrimidines / chemistry*

Substances

  • Carboxylic Acids
  • Pyrimidines
  • Hydrogen
  • pyrimidine