Synthesis and pharmacological evaluation of new flosulide analogues, synthesized from natural safrole

Bioorg Med Chem Lett. 1998 Jan 20;8(2):183-8. doi: 10.1016/s0960-894x(97)10216-5.

Abstract

Four new aryl-sulfonamide derivatives (3a, 4a, 5a-b), having methylenedioxy group attached to phenyl ring, were prepared from natural safrole and evaluated as anti-inflammatory agents. The N-methylsulfonamide 3a and corresponding retrosulfonamide derivative 5a were more active than standards indomethacin and nimesulide, at the same molar concentration, in carrageenan-induced pleurisy assay.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis
  • Anti-Inflammatory Agents, Non-Steroidal / chemistry*
  • Anti-Inflammatory Agents, Non-Steroidal / therapeutic use
  • Cyclooxygenase Inhibitors / chemical synthesis
  • Cyclooxygenase Inhibitors / chemistry*
  • Cyclooxygenase Inhibitors / therapeutic use
  • Disease Models, Animal
  • Drug Evaluation
  • Edema / drug therapy
  • Female
  • Indans / chemical synthesis
  • Indans / chemistry*
  • Indans / therapeutic use
  • Male
  • Pleurisy / drug therapy
  • Rats
  • Safrole / chemistry*

Substances

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase Inhibitors
  • Indans
  • flosulide
  • Safrole