Synthesis and anti-inflammatory activity of 2-aryloxy methyl oxazolines

Bioorg Med Chem Lett. 2008 Aug 15;18(16):4597-601. doi: 10.1016/j.bmcl.2008.07.029. Epub 2008 Jul 15.

Abstract

A series of potential biologically active 2-aryloxy methyl oxazolines 3a-n have been synthesized from substituted hydroxybenzenes 1a-n with good chemical yield. The compounds 3a-n were screened for their anti-inflammatory, ulcerogenic, cyclooxygenase activities and also for their acute toxicity. The potency of the compounds was compared with that of the standard drugs, aspirin and phenyl butazone. The outcome indicates that compounds 3b (48.2%), 3h (48.5%) and 3l (46.5%) offered significant anti-inflammatory activity with low ulcerogenic activity than the standard drugs.

MeSH terms

  • Animals
  • Anti-Inflammatory Agents / chemical synthesis*
  • Anti-Inflammatory Agents / pharmacology*
  • Body Weight
  • Chemistry, Pharmaceutical / methods
  • Drug Design
  • Edema / drug therapy
  • Ethanolamine / chemistry
  • Microsomes / metabolism
  • Microwaves
  • Models, Chemical
  • Oxazoles / chemical synthesis*
  • Oxazoles / pharmacology*
  • Phenylbutazone / pharmacology
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Rats
  • Ulcer / drug therapy

Substances

  • Anti-Inflammatory Agents
  • Oxazoles
  • Ethanolamine
  • Prostaglandin-Endoperoxide Synthases
  • Phenylbutazone