PEG mediated synthesis and pharmacological evaluation of some fluoro substituted pyrazoline derivatives as antiinflammatory and analgesic agents

Bioorg Med Chem Lett. 2013 May 1;23(9):2575-8. doi: 10.1016/j.bmcl.2013.02.105. Epub 2013 Mar 7.

Abstract

A new series of fluoro substituted pyrazoline derivatives 5a-g and 6a-g were synthesized in good to excellent yield from the corresponding pyrazole chalcones, 4a-g, by using polyethylene glycol-400 (PEG-400) as an alternative reaction medium. The newly synthesized compounds were characterized and screened for their in vivo antiinflammatory and analgesic activity. Compounds 5g and 6g were found to be more potent than standard drug Diclofenac and six other compounds 5b, 5c, 5f, 6b, 6c and 6f showed significant antiinflammatory activity as compared to standard drug. Compounds 5c, 5d, 5e, 5f, 6c, 6d, 6e and 6f showed significant analgesic activity as compared to standard drug Aspirin.

Publication types

  • Research Support, Non-U.S. Gov't

MeSH terms

  • Analgesics / chemical synthesis*
  • Analgesics / pharmacology
  • Analgesics / therapeutic use
  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / pharmacology
  • Anti-Inflammatory Agents / therapeutic use
  • Edema / chemically induced
  • Edema / drug therapy
  • Fluorine / chemistry*
  • Polyethylene Glycols / chemistry*
  • Pyrazoles / chemistry*
  • Pyrazoles / pharmacology
  • Pyrazoles / therapeutic use
  • Rats
  • Rats, Wistar
  • Structure-Activity Relationship
  • Tail / drug effects

Substances

  • Analgesics
  • Anti-Inflammatory Agents
  • Pyrazoles
  • Fluorine
  • pyrazole
  • Polyethylene Glycols