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.

中文翻译：

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一类新型四氢苯并噻吩衍生物的设计、合成及抗菌评价

在这项研究中，设计了一系列新的四氢苯并噻吩衍生物。新设计的分子是通过药物化学途径合成的，其表征是通过使用 NMR 和 HR-MS 技术完成的。已对革兰氏阴性和革兰氏阳性细菌进行了合成化合物的生物学评价。市售抗生素如环丙沙星和庆大霉素用作对照。体外评估结果表明，大多数目标化合物在抑制细菌生长方面表现出良好的效力，包括大肠杆菌（ MIC：0.64–19.92 μM）、铜绿假单胞菌（MIC：0.72–45.30 μM）、沙门氏菌（ MIC：0.54–90.58 μM）和金黄色葡萄球菌（MIC：1.11–99.92 μM）。特别是，化合物3b表现出优异的活性，其对大肠杆菌的 MIC 值为 1.11 μM ，对铜绿假单胞菌为 1.00 μM，对沙门氏菌为 0.54 μM ，对金黄色葡萄球菌为1.11 μM 。从结果中，确定了一种有前途的先导化合物用于未来的开发。