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
21 مهر 1401
Accepted
18 آبان 1401
First published
14 آذر 1401

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

To request permission to reproduce material from this article, please go to the Copyright Clearance Center request page.

If you are an author contributing to an RSC publication, you do not need to request permission provided correct acknowledgement is given.

If you are the author of this article, you do not need to request permission to reproduce figures and diagrams provided correct acknowledgement is given. If you want to reproduce the whole article in a third-party publication (excluding your thesis/dissertation for which permission is not required) please go to the Copyright Clearance Center request page.

Read more about how to correctly acknowledge RSC content.

Social activity

Spotlight

Advertisements