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

2019 unpublished
Three series of 2-(4-methylsulfonylphenyl) indole derivatives have been designed and synthesized. The synthesized compounds were evaluated for their antimicrobial, COX inhibitory and antiinflammatory 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 high
more » ... ith high selectivity toward 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 correlated with results of in vitro COX-2 inhibition assays. hydrazone derivatives (7a-k) in good yield. The structure elucidation of hydrazone derivatives (7a-k) was based on IR, 1 H NMR, and 13 C NMR spectral data. IR spectra showed bands at 1593-1597 cm -1 for C=N and disappearance of carbonyl absorption band at 1657-1670 cm -1 which confirm hydrazone formation.
doi:10.21203/rs.2.17036/v1 fatcat:2fc6ecup2jdrpmzsomljxurlpa