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Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were assessed for their antimicrobial, COX inhibitory and anti-inflammatory activities. Compound  7g  was identified to be the most potent antibacterial candidate against strains of  MRSA ,  E. coli, K. pneumoniae, P. aeruginosa,  and  A. baumannii , respectively, with safe therapeutic dose. Compounds  7a–k, 8a–c,  and  9a–c  showed good anti-inflammatory activity with excessive selectivity towards COX-2 in comparison with reference drugs indomethacin and celecoxib. Compounds  9a–c  were found to release moderate amounts of NO to decrease the side effects associated with selective COX-2 inhibitors. A molecular modeling study for compounds  7b, 7h,  and  7i  into COX-2 active site was correlated with the results of in vitro COX-2 inhibition assays.

bmc chemistry

Synthesis and biological evaluation of 2-(4-methylsulfonyl phenyl) indole derivatives: multi-target compounds with dual antimicrobial and anti-inflammatory activities