Design, synthesis and pharmacological evaluation of novel azole derivatives of aryl acetic acid as anti-inflammatory and analgesic agents

Abstract

A series of substituted azole derivatives (3a–e, 4a–e and 5a–e) were synthesised by the cyclisation of N¹(diphenylethanoyl)-N⁴-substituted phenyl thiosemicarbazides under various reaction conditions. These compounds were tested in vivo for their anti-inflammatory activity. The compounds which showed activity comparable to the standard drug ibuprofen, were screened for their analgesic, ulcerogenic and lipid peroxidation activities. The compounds 5-(diphenylmethyl)-N-(4-fluorophenyl)-1,3,4-oxadiazol-2-amine (3b) and 5-(diphenylmethyl)-N-(3-chloro-4-fluorophenyl)-1,3,4-oxadiazol-2-amine (3c) emerged as the most active compounds of the series, and were moderately more potent than the standard drug, ibuprofen. (This abstract was published in Inflammation Research, Supplement 2, Volume 56, page A101, 2008.)

Keywords::

• Diphenyl acetic acids
• anti-inflammatory
• analgesic
• acute ulcerogenicity
• lipid peroxidation

Acknowledgements

The authors would like to thank the Central Drug Research Institute (CDRI) and the Central Instrumentation Facility (CIF), Hamdard University for the spectral analysis of the compounds. The authors would also like to thank Shaukat Shah, (in-charge of the animal house) and Jamia Hamdard for providing the Wistar rats.

Declaration of interest

The authors report no conflicts of interest. The authors alone are responsible for the content and writing of the paper.