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.

中文翻译：

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2-（4-甲基磺酰基苯基）吲哚衍生物的合成和生物学评估：具有双重抗菌和消炎作用的多目标化合物

已经设计并合成了三个系列的2-（4-甲基磺酰基苯基）吲哚衍生物。评估合成的化合物的抗微生物，COX抑制和抗炎活性。化合物7g经鉴定为分别以安全治疗剂量针对MRSA，大肠杆菌，肺炎克雷伯菌，铜绿假单胞菌和鲍曼不动杆菌菌株的最有效的候选抗菌剂。与参考药物消炎痛和塞来昔布相比，化合物7a-k，8a-c和9a-c具有良好的抗炎活性，并且对COX-2的选择性过高。发现化合物9a–c释放适量的NO，以减少与选择性COX-2抑制剂相关的副作用。化合物7b，7h，