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Molecules 2012, 17(2), 1751-1763; doi:10.3390/molecules17021751
Article

Design, Synthesis and Preliminary Pharmacological Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having a 4-(Methylsulfonyl) Aniline Pharmacophore

1,* , 1 and 2
1 Department of Pharmaceutical Chemistry, College of Pharmacy, University of Baghdad, Baghdad, 10047, Iraq 2 Department of Pharmaceutical Chemistry, College of Pharmacy, University of Kufa, Najaf, 54001, Iraq
* Author to whom correspondence should be addressed.
Received: 30 December 2011 / Revised: 20 January 2012 / Accepted: 20 January 2012 / Published: 10 February 2012
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Abstract

A series of 4-(methylsulfonyl)aniline derivatives were synthesized in order to obtain new compounds as a potential anti-inflammatory agents with expected selectivity against COX-2 enzyme. In vivo acute anti-inflammatory activity of the final compounds 1114 was evaluated in rat using an egg-white induced edema model of inflammation in a dose equivalent to 3 mg/Kg of diclofenac sodium. All tested compounds produced significant reduction of paw edema with respect to the effect of propylene glycol 50% v/v (control group). Moreover, the activity of compounds 11 and 14 was significantly higher than that of diclofenac sodium (at 3 mg/Kg) in the 120–300 minute time interval, while compound 12 expressed a comparable effect to that of diclofenac sodium in the 60–240 minute time interval time, and compound 13 showed a comparable effect to that of diclofenac sodium at all experimental times. The result of this study indicates that the incorporation of the 4-(methylsulfonyl)aniline pharamacophore into naproxen, indomethacine, diclofenac and mefanamic acid maintained their anti-inflammatory activity and may increase selectivity towards the COX-2 enzyme which will be confirmed in the future by assessing COX-2: COX-1 inhibitory ratios using a whole blood assay.
Keywords: anti-inflammatory; paw edema; NSAIDs; naproxen; indomethacin; mefanamic acid; diclofenac anti-inflammatory; paw edema; NSAIDs; naproxen; indomethacin; mefanamic acid; diclofenac
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Mahdi, M.F.; Mohammed, M.H.; Jassim, A.A.K. Design, Synthesis and Preliminary Pharmacological Evaluation of New Non-Steroidal Anti-Inflammatory Agents Having a 4-(Methylsulfonyl) Aniline Pharmacophore. Molecules 2012, 17, 1751-1763.

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