A study of anti-inflammatory activity of some novel alpha-amino naphthalene and beta-amino naphthalene derivatives

Arch Pharm (Weinheim). 2006 Mar;339(3):145-52. doi: 10.1002/ardp.200500215.

Abstract

In the present study, some naphthalene derivatives have been synthesized by incorporating azetidinyl and thiazolidinyl moieties at its alpha- or beta-positions such as alpha-(3-chloro-2-oxo-4-substituted)aryl-1-azetidinyl)naphthalenes 6-10, alpha-((substituted)aryl-4-oxo-1,3-thiazolidin-3-yl)naphthalenes 11-15, beta-(3-chloro-2-oxo-4-substituted aryl-1-azetidinyl)naphthalenes 21-25, and beta-(substituted aryl-4-oxo-1,3-thiazolidin-3-yl)naphthalenes 26-30. These compounds have also been screened for acute toxicity and anti-inflammatory and analgesic activities. Compounds which showed better anti-inflammatory and analgesic activities were also examined for their ulcerogenic liability and underwent a cyclooxygenase assay. Two compounds, 12 and 28, were found to exhibit potent anti-inflammatory activity as compared to the standard drugs phenylbutazone and naproxen.

MeSH terms

  • Analgesics / chemical synthesis*
  • Analgesics / toxicity
  • Animals
  • Anti-Inflammatory Agents, Non-Steroidal / chemical synthesis*
  • Anti-Inflammatory Agents, Non-Steroidal / toxicity
  • Female
  • Lethal Dose 50
  • Male
  • Naphthalenes / chemical synthesis*
  • Naphthalenes / toxicity
  • Pain Measurement
  • Peptic Ulcer / chemically induced
  • Prostaglandin-Endoperoxide Synthases / metabolism
  • Rabbits
  • Rats
  • Structure-Activity Relationship

Substances

  • Analgesics
  • Anti-Inflammatory Agents, Non-Steroidal
  • Naphthalenes
  • Prostaglandin-Endoperoxide Synthases