Synthesis, analgesic, anti-inflammatory and anti-ulcerogenic activities of certain novel Schiff's bases as fenamate isosteres

Ahmed M. Alafeefy, Mohammed A. Bakht, Majid A. Ganaie, Mohd N. Ansarie, Nahed N. El-Sayed, Amani S. Awaad

Research output: Contribution to journalArticlepeer-review

65 Scopus citations

Abstract

A series of certain novel Schiff bases as fenamate isosteres (VI:a-k) were synthesized to locate analgesic, anti-inflammatory agent with minimal ulcerogenic potential. The structures of the newly synthesized compounds were elucidated on the basis of their elemental analysis as well as IR, and NMR and mass spectroscopic data. All the compounds were evaluated for their anti-inflammatory activity by carrageenan induced paw oedema method. The compounds possessing good anti-inflammatory activity were further tested for analgesic, ulcerogenic, lipid peroxidation potentials and liver toxicity. Compounds (VI-c), (VI-f), (VI-h) and (VI-i) showed the best anti-inflammatory and significant analgesic activities at doses comparable to that of the standard drug Indomethacin. However, compounds (VI-c) and (VI-f) could be considered the most potent anti-inflammatory and analgesic molecules with maximum reduction in gastro-intestinal ulceration with no hepatocyte necrosis or liver degeneration.

Original languageEnglish
Pages (from-to)179-183
Number of pages5
JournalBioorganic and Medicinal Chemistry Letters
Volume25
Issue number2
DOIs
StatePublished - 15 Jan 2015

Keywords

  • Analgesic
  • Anti-inflammatory
  • Anti-ulcerogenic
  • Fenamate isostere
  • Schiff's bases
  • Synthesis

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