Issue 1, 2023

Design, synthesis and antibacterial evaluation of a novel class of tetrahydrobenzothiophene derivatives

Abstract

In this study, a new series of tetrahydrobenzothiophene derivatives have been designed. Newly designed molecules have been synthesized through a medicinal chemistry route, and their characterization was done by using NMR and HR-MS techniques. Biological evaluation of the synthesized compounds has been done on Gram-negative and Gram-positive bacteria. The marketed antibiotics such as ciprofloxacin and gentamicin were used as controls. The in vitro evaluation results have shown that most of the targeted compounds exhibit good potency in inhibiting the growth of bacteria, including E. coli (MIC: 0.64–19.92 μM), P. aeruginosa (MIC: 0.72–45.30 μM), Salmonella (MIC: 0.54–90.58 μM) and S. aureus (MIC: 1.11–99.92 μM). In particular, compound 3b showed excellent activity with an MIC value of 1.11 μM against E. coli, 1.00 μM against P. aeruginosa, 0.54 μM against Salmonella, and 1.11 μM against S. aureus. From the results, a promising lead compound was identified for future development.

Graphical abstract: Design, synthesis and antibacterial evaluation of a novel class of tetrahydrobenzothiophene derivatives

Supplementary files

Article information

Article type
Research Article
Submitted
13 Okt. 2022
Accepted
09 Nov. 2022
First published
05 Dec. 2022

RSC Med. Chem., 2023,14, 166-172

Design, synthesis and antibacterial evaluation of a novel class of tetrahydrobenzothiophene derivatives

L. Lai, J. Yang, W. Sun, X. Su, J. Chen, X. Chen and S. Pei, RSC Med. Chem., 2023, 14, 166 DOI: 10.1039/D2MD00373B

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