Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents

作者全名："Pei, Shuchen; Lai, Lin; Sun, Wanlin; Lu, Zhaoyang; Hao, Jielei; Liu, Yuheng; Wu, Wen; Guan, Shan; Su, Xiaoyan"

作者地址："[Pei, Shuchen; Lai, Lin; Sun, Wanlin; Lu, Zhaoyang; Hao, Jielei; Su, Xiaoyan] Chongqing Univ Sci & Technol, Coll Chem & Chem Engn, Chongqing 401331, Peoples R China; [Wu, Wen] Chongqing Med & Pharmaceut Coll, Chongqing Engn Res Ctr Pharmaceut Sci, Chongqing Key Lab High Act Tradit Chinese Drug Del, Chongqing 404120, Peoples R China; [Liu, Yuheng; Guan, Shan] Third Mil Med Univ, Natl Engn Res Ctr Immunol Prod, Chongqing 400038, Peoples R China; [Liu, Yuheng] Chongqing Med Univ, Coll Pharm, Dept Pharmacol, Chongqing 400016, Peoples R China"

通信作者："Pei, SC (通讯作者)，Chongqing Univ Sci & Technol, Coll Chem & Chem Engn, Chongqing 401331, Peoples R China.; Wu, W (通讯作者)，Chongqing Med & Pharmaceut Coll, Chongqing Engn Res Ctr Pharmaceut Sci, Chongqing Key Lab High Act Tradit Chinese Drug Del, Chongqing 404120, Peoples R China.; Guan, S (通讯作者)，Third Mil Med Univ, Natl Engn Res Ctr Immunol Prod, Chongqing 400038, Peoples R China."

来源：BIOORGANIC CHEMISTRY

ESI学科分类：BIOLOGY & BIOCHEMISTRY

WOS号：WOS:001102599200001

JCR分区：Q1

影响因子：5.1

年份：2024

卷号：142

期号：　

开始页：　

结束页：　

文献类型：Article

关键词：Tetrahydrobenzothiophene; Antibacterial; Drug desigen; Synthesis

摘要："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 evalu-ated. 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."

基金机构："Scientific Technological Research Program of Chongqing Municipal Education Commission [KJQN201901501]; National Natural Science Foundation of China (NSFC) [82173764]; major project of Study on Pathogenesis and Epidemic Prevention Technology System [2021YFC2302500]; Natural Science Foundation of Chongqing [cstc2021jcyj-msxmX0136, CSTB2022NSCQ-MSX0474]; Postgraduate Innovation Program of Chongqing University of Science and Technology [YKJCX2320510]"

基金资助正文："This research was funded by the Scientific Technological Research Program of Chongqing Municipal Education Commission (No. KJQN201901501) , the National Natural Science Foundation of China (NSFC, No. 82173764) , the major project of Study on Pathogenesis and Epidemic Prevention Technology System (No. 2021YFC2302500) , the Natural Science Foundation of Chongqing (cstc2021jcyj-msxmX0136, CSTB2022NSCQ-MSX0474) , and the Postgraduate Innovation Program of Chongqing University of Science and Technology (No. YKJCX2320510) ."