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 11–14 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.
Highlights
Non-steroidal anti-inflammatory drugs (NSAIDs) are used to treat a wide variety of illnesses and diseases, including inflammation [1], cancers [2], diabetes [3]; and diseases of the peripheral and central nervous system, e.g., Alzheimer’s and Parkinson’s [4]
The anti-inflammatory effect of NSAIDs arises from their ability to inhibiting cyclooxygenase (COX) enzyme [1]
Three different COX enzymes exist, known as COX-1, COX-2 and COX-3, COX-1 is a constitutive isoform found in most normal cells and tissues [6]
Summary
Non-steroidal anti-inflammatory drugs (NSAIDs) are used to treat a wide variety of illnesses and diseases, including inflammation [1], cancers [2], diabetes [3] (insulin-resistant and related metabolic syndrome); and diseases of the peripheral and central nervous system, e.g., Alzheimer’s and Parkinson’s [4]. This versatility is attributed to a wide variety of effects of these drugs on cell function. The anti-inflammatory effect of NSAIDs arises from their ability to inhibiting cyclooxygenase (COX) enzyme [1]. There is still a need for new, selective COX-2 inhibitors with an improved safety profile
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