A series of 2-(4-(methylsulfonyl)phenyl)-1-substituted-indole derivatives 4a-f was designed and synthesized as indomethacin analogs; All compounds were evaluated for their in vitro COX-2 inhibitory activity as well as in vivo anti-inflammatory activity using indomethacin as reference drug. All synthesized compounds showed good anti-inflammatory activity and more selectivity for COX-2 inhibition. Molecular modeling study is performed and the results were in agreement with that obtained from in vitro COX-2 inhibition assays.
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