SYNTHESIS AND BIOLOGICAL EVALUATION OF NOVEL CHALCONES WITH METHANE-SULFONYL END AS POTENT ANALGESIC AND ANTI-INFLAMMATORY AGENTS

In the present study, eleven new chalcones bearing a methanesulfonyl group at para position have been synthesized by the condensation of 4-methylsulphonylacetophenone with different para-substituted aromatic aldehydes. The structures of the newly synthesized molecules were elucidated by spectroscopic methods such as as¹H NMR, ¹³C NMR, and mass. These compounds were screened for their anti-inflammatory activity by carrageenan-induced rat paw edema and leucocytes migration methods and analgesic activity by acetic acid-induced writhing test in albino Wistar rats. Among the synthesized compounds, MS7 to MS10 which contain electron-withdrawing groups were found to be most active with reference to anti-inflammatory activity at a dose level of 10 mg/kg and caused a significant reduction in the number of recruited leukocytes and inhibition of pleural exudates formation that was comparable to that of indomethacin at a dose of 10 mg/kg. The compounds which contain halogens and methoxy groups showed a significant analgesic activity at a dose of 10 mg/kg when compared to standard diclofenac sodium. Thus, it can be concluded that among the compounds tested, the ones with halogens possess significant anti-inflammatory and analgesic activity in rats. Further studies involving the investigations of the biochemical pathways may result in the identification of lead with potent anti-inflammatory and analgesic activity and with low toxicity and better therapeutic index.