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Design, Synthesis and Anti-Bacterial Evaluation of Tetrahydrobenzothiophene Derivatives as lipopolysaccharide biogenesis inhibitors.



Bacterial infections caused by multidrug resistant bacteria has emerged as major threats to human communities worldwide. There is a great need to develop new mechanisms by which antibacterial agents can combat bacterial antibiotic resistance. Objective: It is an aim to synthesize and characterize a series of novel tetrahydrobenzothiophene derivatives and evaluated for their antibacterial activities.



In this study, we have synthesized 2-benzamido-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid derivatives (3a-3r) and investigated their antibacterial activities against E. coli, P. aeruginosa, Salmonella, and S. aureus.



The MIC values demonstrated that all synthesized derivatives possessed potent antibacterial activity properties. Compounds 3b, 3e, 3f, 3g, 3h, 3n, and 3q exhibited in vitro excellent antibacterial efficiency. Compounds 3b, 3e, 3f, and 3p were evaluated for their in vitro time-kill assay displayed concentration-dependent bacteriostatic effects. Compounds 3b, 3e, 3f, and 3p showed moderate water solubility, high stability in plasma, and moderate acute oral toxicity.



Most of the 2-benzamido-4,5,6,7-tetrahydrobenzo[b]thiophene-3-carboxylic acid derivatives exhibited potent antibacterial activities. The data reported in this paper may guide the design of tetrahydrobenzothiophene derivatives.
