Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents

[Display omitted] •Novel tetrahydrobenzothiophene antibacterial compounds were designed and synthesized.•Compound 6p holds promise as a potential therapeutic agent for combating bacterial infections.•The structure–activity relationship of tetrahydrobenzothiophene antibacterial molecules was studied....

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Veröffentlicht in:Bioorganic chemistry 2024-01, Vol.142, p.106932-106932, Article 106932
Hauptverfasser: Lai, Lin, Sun, Wanlin, Lu, Zhaoyang, Su, Xiaoyan, Hao, Jielei, Liu, Yuheng, Wu, Wen, Guan, Shan, Pei, Shuchen
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container_end_page 106932
container_issue
container_start_page 106932
container_title Bioorganic chemistry
container_volume 142
creator Lai, Lin
Sun, Wanlin
Lu, Zhaoyang
Su, Xiaoyan
Hao, Jielei
Liu, Yuheng
Wu, Wen
Guan, Shan
Pei, Shuchen
description [Display omitted] •Novel tetrahydrobenzothiophene antibacterial compounds were designed and synthesized.•Compound 6p holds promise as a potential therapeutic agent for combating bacterial infections.•The structure–activity relationship of tetrahydrobenzothiophene antibacterial molecules was studied.•The molecules are designed to inhibit a wide variety of bacteria.•The compound has a better healing effect on the skin. 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.
doi_str_mv 10.1016/j.bioorg.2023.106932
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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. 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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. 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subjects Animals
Anti-Bacterial Agents - pharmacology
Anti-Infective Agents - pharmacology
Antibacterial
Bacteria
Drug desigen
Humans
Mice
Microbial Sensitivity Tests
Synthesis
Tetrahydrobenzothiophene
title Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents
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