Improving the solubility of a new class of antiinflammatory pharmacodynamic hybrids, that release nitric oxide and inhibit cycloxygenase-2 isoenzyme

Eur J Med Chem. 2012 Dec:58:287-98. doi: 10.1016/j.ejmech.2012.10.014. Epub 2012 Oct 18.

Abstract

The development of a novel class of pharmacodynamic hybrids that inhibits COX-2 isoform is reported. These molecules display enhanced nitric oxide releasing properties due to the presence of an ionisable moiety. The in vivo analgesic/anti-inflammatory activity was maintained in relation to the parent compounds.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Acetic Acid
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacokinetics
  • Anti-Inflammatory Agents, Non-Steroidal / pharmacology*
  • Carrageenan / antagonists & inhibitors
  • Carrageenan / pharmacology
  • Constriction, Pathologic / chemically induced
  • Constriction, Pathologic / drug therapy*
  • Cyclooxygenase 2 / metabolism*
  • Dose-Response Relationship, Drug
  • Enzyme Inhibitors / chemistry*
  • Enzyme Inhibitors / pharmacokinetics
  • Enzyme Inhibitors / pharmacology*
  • Isoenzymes / antagonists & inhibitors
  • Isoenzymes / metabolism
  • Male
  • Mice
  • Molecular Structure
  • Muscle, Smooth, Vascular / chemistry
  • Muscle, Smooth, Vascular / drug effects
  • Muscle, Smooth, Vascular / metabolism
  • Nitric Oxide / metabolism*
  • Rats
  • Rats, Sprague-Dawley
  • Rats, Wistar
  • Solubility
  • Structure-Activity Relationship

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Enzyme Inhibitors
  • Isoenzymes
  • Nitric Oxide
  • Carrageenan
  • Cyclooxygenase 2
  • Acetic Acid