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Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents
Bioorganic Chemistry ( IF 4.5 ) Pub Date : 2023-10-21 , DOI: 10.1016/j.bioorg.2023.106932
Shuchen Pei 1 , Lin Lai 1 , Wanlin Sun 1 , Zhaoyang Lu 1 , Jielei Hao 1 , Yuheng Liu 2 , Wen Wu 3 , Shan Guan 4 , Xiaoyan Su 1
Affiliation  

The incidence of infections caused by drug-resistant bacteria has been one of the most serious health threats in the past and is substantially increasing in an alarming rate. Therefore, the development of new antimicrobial agents to combat bacterial resistance effectively is urgent. This study focused on the design and synthesis of 40 novel tetrahydrobenzothiophene amide/sulfonamide derivatives and their antibacterial activities were evaluated. Compounds 2p, 6p, and 6 s exhibited significant inhibitory effects on the growth of bacteria. To assess their safety, the cytotoxicity of the compounds was assessed using human normal liver cells, revealing that compound 6p has lower cytotoxicity. A mouse wound healing experiment demonstrated that compound 6p effectively improved wound infection induced by trauma and accelerated the healing process. Compound 6p holds promise as a potential therapeutic agent for combating bacterial infections.



中文翻译:

发现新型四氢苯并噻吩衍生物作为抗菌药物的 MSBA 抑制剂

耐药细菌引起的感染的发生率在过去一直是最严重的健康威胁之一,并且正在以惊人的速度大幅增加。因此,开发新型抗菌药物来有效对抗细菌耐药性刻不容缓。本研究重点设计和合成了40种新型四氢苯并噻吩酰胺/磺酰胺衍生物,并对其抗菌活性进行了评价。化合物2p6p6s对细菌的生长表现出显着的抑制作用。为了评估其安全性,使用人类正常肝细胞评估了化合物的细胞毒性,结果表明化合物6p具有较低的细胞毒性。小鼠伤口愈合实验表明,化合物6p能有效改善外伤引起的伤口感染,加速愈合过程。化合物6p有望成为对抗细菌感染的潜在治疗剂。

更新日期:2023-10-21
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