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 |
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container_title | Bioorganic chemistry |
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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 |
format | Article |
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•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.</description><identifier>ISSN: 0045-2068</identifier><identifier>EISSN: 1090-2120</identifier><identifier>DOI: 10.1016/j.bioorg.2023.106932</identifier><identifier>PMID: 37913586</identifier><language>eng</language><publisher>United States: Elsevier Inc</publisher><subject>Animals ; Anti-Bacterial Agents - pharmacology ; Anti-Infective Agents - pharmacology ; Antibacterial ; Bacteria ; Drug desigen ; Humans ; Mice ; Microbial Sensitivity Tests ; Synthesis ; Tetrahydrobenzothiophene</subject><ispartof>Bioorganic chemistry, 2024-01, Vol.142, p.106932-106932, Article 106932</ispartof><rights>2023</rights><rights>Copyright © 2023 Elsevier Inc. All rights reserved.</rights><lds50>peer_reviewed</lds50><woscitedreferencessubscribed>false</woscitedreferencessubscribed><citedby>FETCH-LOGICAL-c362t-a23587225a2deaee2a7b4a9d1efaa7a09e81a457753b0b22f8be93b253e544613</citedby><cites>FETCH-LOGICAL-c362t-a23587225a2deaee2a7b4a9d1efaa7a09e81a457753b0b22f8be93b253e544613</cites></display><links><openurl>$$Topenurl_article</openurl><openurlfulltext>$$Topenurlfull_article</openurlfulltext><thumbnail>$$Tsyndetics_thumb_exl</thumbnail><link.rule.ids>314,780,784,27924,27925</link.rule.ids><backlink>$$Uhttps://www.ncbi.nlm.nih.gov/pubmed/37913586$$D View this record in MEDLINE/PubMed$$Hfree_for_read</backlink></links><search><creatorcontrib>Lai, Lin</creatorcontrib><creatorcontrib>Sun, Wanlin</creatorcontrib><creatorcontrib>Lu, Zhaoyang</creatorcontrib><creatorcontrib>Su, Xiaoyan</creatorcontrib><creatorcontrib>Hao, Jielei</creatorcontrib><creatorcontrib>Liu, Yuheng</creatorcontrib><creatorcontrib>Wu, Wen</creatorcontrib><creatorcontrib>Guan, Shan</creatorcontrib><creatorcontrib>Pei, Shuchen</creatorcontrib><title>Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents</title><title>Bioorganic chemistry</title><addtitle>Bioorg Chem</addtitle><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.</description><subject>Animals</subject><subject>Anti-Bacterial Agents - pharmacology</subject><subject>Anti-Infective Agents - pharmacology</subject><subject>Antibacterial</subject><subject>Bacteria</subject><subject>Drug desigen</subject><subject>Humans</subject><subject>Mice</subject><subject>Microbial Sensitivity Tests</subject><subject>Synthesis</subject><subject>Tetrahydrobenzothiophene</subject><issn>0045-2068</issn><issn>1090-2120</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2024</creationdate><recordtype>article</recordtype><sourceid>EIF</sourceid><recordid>eNp9kE9v2zAMxYWhw5K2-wZDoWMvTvXHsuxLgTZb2wEddth6FiibThQ4ViYpAbJPPwXueuyJBPEe-fgj5AtnC854dbNZWOd9WC0EEzKPqkaKD2TOWcMKwQU7I3PGSlUIVtUzch7jhjHOS119IjOpGy5VXc1J-9XF1h8wHKnv6Zi7gSZMAdbHLniL41-f1s7v1jgi7TC4AyR3wEgh0h-_7u-oG9fOuuRDpL0PFMbktq7NVgcDhRWOKV6Sjz0MET-_1gvy8vDt9_KpeP75-H1591y0shKpAJEjaSEUiA4BUYC2JTQdxx5AA2uw5lAqrZW0zArR1xYbaYWSqMqy4vKCXE97d8H_2WNMZpufw2GAEf0-GlHXSkmt9ElaTtKcNMaAvdkFt4VwNJyZE16zMRNec8JrJrzZdvV6YW-32L2Z_vPMgttJgPnPg8NgYutwbLFzAdtkOu_ev_AP3_CPSQ</recordid><startdate>202401</startdate><enddate>202401</enddate><creator>Lai, Lin</creator><creator>Sun, Wanlin</creator><creator>Lu, Zhaoyang</creator><creator>Su, Xiaoyan</creator><creator>Hao, Jielei</creator><creator>Liu, Yuheng</creator><creator>Wu, Wen</creator><creator>Guan, Shan</creator><creator>Pei, Shuchen</creator><general>Elsevier Inc</general><scope>CGR</scope><scope>CUY</scope><scope>CVF</scope><scope>ECM</scope><scope>EIF</scope><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7X8</scope></search><sort><creationdate>202401</creationdate><title>Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents</title><author>Lai, Lin ; Sun, Wanlin ; Lu, Zhaoyang ; Su, Xiaoyan ; Hao, Jielei ; Liu, Yuheng ; Wu, Wen ; Guan, Shan ; Pei, Shuchen</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c362t-a23587225a2deaee2a7b4a9d1efaa7a09e81a457753b0b22f8be93b253e544613</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2024</creationdate><topic>Animals</topic><topic>Anti-Bacterial Agents - pharmacology</topic><topic>Anti-Infective Agents - pharmacology</topic><topic>Antibacterial</topic><topic>Bacteria</topic><topic>Drug desigen</topic><topic>Humans</topic><topic>Mice</topic><topic>Microbial Sensitivity Tests</topic><topic>Synthesis</topic><topic>Tetrahydrobenzothiophene</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Lai, Lin</creatorcontrib><creatorcontrib>Sun, Wanlin</creatorcontrib><creatorcontrib>Lu, Zhaoyang</creatorcontrib><creatorcontrib>Su, Xiaoyan</creatorcontrib><creatorcontrib>Hao, Jielei</creatorcontrib><creatorcontrib>Liu, Yuheng</creatorcontrib><creatorcontrib>Wu, Wen</creatorcontrib><creatorcontrib>Guan, Shan</creatorcontrib><creatorcontrib>Pei, Shuchen</creatorcontrib><collection>Medline</collection><collection>MEDLINE</collection><collection>MEDLINE (Ovid)</collection><collection>MEDLINE</collection><collection>MEDLINE</collection><collection>PubMed</collection><collection>CrossRef</collection><collection>MEDLINE - Academic</collection><jtitle>Bioorganic chemistry</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Lai, Lin</au><au>Sun, Wanlin</au><au>Lu, Zhaoyang</au><au>Su, Xiaoyan</au><au>Hao, Jielei</au><au>Liu, Yuheng</au><au>Wu, Wen</au><au>Guan, Shan</au><au>Pei, Shuchen</au><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Discovery of novel tetrahydrobenzothiophene derivatives as MSBA inhibitors for antimicrobial agents</atitle><jtitle>Bioorganic chemistry</jtitle><addtitle>Bioorg Chem</addtitle><date>2024-01</date><risdate>2024</risdate><volume>142</volume><spage>106932</spage><epage>106932</epage><pages>106932-106932</pages><artnum>106932</artnum><issn>0045-2068</issn><eissn>1090-2120</eissn><abstract>[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.</abstract><cop>United States</cop><pub>Elsevier Inc</pub><pmid>37913586</pmid><doi>10.1016/j.bioorg.2023.106932</doi><tpages>1</tpages></addata></record> |
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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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