Abstract

Rajib Kumar Singh^1,2, Arvind Kumar¹ and Arun K. Mishra^1*

DOI : http://dx.doi.org/10.13005/ojc/370629

The purpose of the present research was to synthesize a new series of acetanilide derivatives that would have analgesic and anti-inflammatory properties in laboratory animals (rats). IR spectroscopy, 1HNMR spectroscopy and Mass spectroscopy were used to confirm the structures of freshly synthesised compounds. The goal of the computer analysis of synthesized compounds was to see how similar they were in terms of physicochemical properties. For this, physiochemical parameters were calculated. The result suggested the reasonable physiochemical similarity with diclofenac sodium and Indomethacin. Molecular docking studies showed that the all the test compounds perfectly docked with COX-2 enzyme with all the drug-likeness characteristics. Before start of in-vivo evaluation, in vitro cyclooxygenase (COX) inhibition assays was performed with an aim to evaluate the compounds against the protein target COX-2 which would exhibit their inhibitory activity. The test compounds (C1-C6) were subjected to analgesic activity evaluation by Eddy’s hot plate method and anti-inflammatory activity evaluation by Carageenan induced edema method respectively.
Compound C6 [Methyl 2-(2-oxo-2-(p-tolylamino)ethoxy)benzoate] showed highest anti-inflammatory response (61.36 %) at 120 m, which was quite analogous with the positive control. The response of promising compounds C5 [2-phenoxy-N-(o-tolyl)acetamide] showed the highest analgesic action.
The result concluded that out of all the synthesized compounds, compound C5 and C6 could be used as promising new lead molecules to treat pain and inflammation respectively.

Acetanilide; Anti-Inflammatory; Analgesic; NSAID; Phenoxyacetanilide; Structure-Activity Relationships

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