Introducing Broadened Antibacterial Activity to Rhodanine Derivatives Targeting Enoyl-Acyl Carrier Protein Reductase
Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections i...
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| Veröffentlicht in: | Chemical & pharmaceutical bulletin 2019/02/01, Vol.67(2), pp.125-129 |
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| container_title | Chemical & pharmaceutical bulletin |
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| creator | Sun, Zhi-Gang Xu, Yun-Jie Xu, Jian-Fei Liu, Qi-Xing Yang, Yu-Shun Zhu, Hai-Liang |
| description | Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50 = 3.18 µM for Mtb InhA; IC50 = 10 nM for DNA Gyrase B) with positive controls. Structure–activity relationship discussion and molecular docking model revealed the significance of rhodanine moiety and derived methoxyl on meta-position, pointing out orientations for future modification. |
| doi_str_mv | 10.1248/cpb.c18-00663 |
| format | Article |
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This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50 = 3.18 µM for Mtb InhA; IC50 = 10 nM for DNA Gyrase B) with positive controls. 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Pharm. Bull.</addtitle><description>Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50 = 3.18 µM for Mtb InhA; IC50 = 10 nM for DNA Gyrase B) with positive controls. Structure–activity relationship discussion and molecular docking model revealed the significance of rhodanine moiety and derived methoxyl on meta-position, pointing out orientations for future modification.</description><subject>Acyl carrier protein</subject><subject>Antibacterial activity</subject><subject>bacterial infection</subject><subject>Biological activity</subject><subject>computer assistant drug design</subject><subject>Deoxyribonucleic acid</subject><subject>Derivatives</subject><subject>DNA</subject><subject>DNA Gyrase B</subject><subject>DNA topoisomerase</subject><subject>enoyl-acyl carrier protein reductase</subject><subject>Molecular docking</subject><subject>Molecular structure</subject><subject>Proteins</subject><subject>Reductase</subject><subject>rhodanine</subject><subject>Tuberculosis</subject><issn>0009-2363</issn><issn>1347-5223</issn><fulltext>true</fulltext><rsrctype>article</rsrctype><creationdate>2019</creationdate><recordtype>article</recordtype><recordid>eNpdkc1rGzEQxUVpady0x16LoJdeNtHHSto9uk6aBgItIT0LrTS2ZdaSK8kB__fVxqkDucwwvB9vhnkIfabkgrK2u7S74cLSriFESv4GzShvVSMY42_RjBDSN4xLfoY-5LwhhAmi-Ht0xominCk2Q-U2lBTd3vqwwt9TNA4CODwPxQ_GFkjejHhui3_05YBLxPfr6EzwAfBVFR9NVSDjB5NWUCaP6xAPYzO3hxEvTEoeEv6dYgEf8D3UPcVk-IjeLc2Y4dNzP0d_flw_LH42d79ubhfzu8ZK0ZXGKUUcbSUfCFFqKaSyklFDSecoFU7WuR0kJ1bIthcO-MBhmGoLXNih5-fo29F3l-LfPeSitz5bGEcTIO6zZlT1gtOekop-fYVu4j6Fep2uv6Sd6qSSlWqOlE0x5wRLvUt-a9JBU6KnOHSNQ9c49FMclf_y7LoftuBO9P__V-DmCFTVWzPGMNbXvuy2Wdk1bL1mhPaTqSKsNqUJZWIqPWdUdIxWp8XRaZOLWcFplUnF2xGeDpNKs6mcDnxR1yZpCPwfrOq0WQ</recordid><startdate>20190201</startdate><enddate>20190201</enddate><creator>Sun, Zhi-Gang</creator><creator>Xu, Yun-Jie</creator><creator>Xu, Jian-Fei</creator><creator>Liu, Qi-Xing</creator><creator>Yang, Yu-Shun</creator><creator>Zhu, Hai-Liang</creator><general>The Pharmaceutical Society of Japan</general><general>Pharmaceutical Society of Japan</general><general>Japan Science and Technology Agency</general><scope>NPM</scope><scope>AAYXX</scope><scope>CITATION</scope><scope>7TK</scope><scope>7TM</scope><scope>7U9</scope><scope>H94</scope><scope>7X8</scope></search><sort><creationdate>20190201</creationdate><title>Introducing Broadened Antibacterial Activity to Rhodanine Derivatives Targeting Enoyl-Acyl Carrier Protein Reductase</title><author>Sun, Zhi-Gang ; Xu, Yun-Jie ; Xu, Jian-Fei ; Liu, Qi-Xing ; Yang, Yu-Shun ; Zhu, Hai-Liang</author></sort><facets><frbrtype>5</frbrtype><frbrgroupid>cdi_FETCH-LOGICAL-c658t-d770d1463b0077f567c621a108d115d667c4b630c56495de3b3ebe3b34e35cb93</frbrgroupid><rsrctype>articles</rsrctype><prefilter>articles</prefilter><language>eng</language><creationdate>2019</creationdate><topic>Acyl carrier protein</topic><topic>Antibacterial activity</topic><topic>bacterial infection</topic><topic>Biological activity</topic><topic>computer assistant drug design</topic><topic>Deoxyribonucleic acid</topic><topic>Derivatives</topic><topic>DNA</topic><topic>DNA Gyrase B</topic><topic>DNA topoisomerase</topic><topic>enoyl-acyl carrier protein reductase</topic><topic>Molecular docking</topic><topic>Molecular structure</topic><topic>Proteins</topic><topic>Reductase</topic><topic>rhodanine</topic><topic>Tuberculosis</topic><toplevel>peer_reviewed</toplevel><toplevel>online_resources</toplevel><creatorcontrib>Sun, Zhi-Gang</creatorcontrib><creatorcontrib>Xu, Yun-Jie</creatorcontrib><creatorcontrib>Xu, Jian-Fei</creatorcontrib><creatorcontrib>Liu, Qi-Xing</creatorcontrib><creatorcontrib>Yang, Yu-Shun</creatorcontrib><creatorcontrib>Zhu, Hai-Liang</creatorcontrib><creatorcontrib>aState Key Laboratory of Pharmaceutical Biotechnology</creatorcontrib><creatorcontrib>Linyi Central Hospital</creatorcontrib><creatorcontrib>Nanjing University</creatorcontrib><creatorcontrib>bCentral Laboratory</creatorcontrib><collection>PubMed</collection><collection>CrossRef</collection><collection>Neurosciences Abstracts</collection><collection>Nucleic Acids Abstracts</collection><collection>Virology and AIDS Abstracts</collection><collection>AIDS and Cancer Research Abstracts</collection><collection>MEDLINE - Academic</collection><jtitle>Chemical & pharmaceutical bulletin</jtitle></facets><delivery><delcategory>Remote Search Resource</delcategory><fulltext>fulltext</fulltext></delivery><addata><au>Sun, Zhi-Gang</au><au>Xu, Yun-Jie</au><au>Xu, Jian-Fei</au><au>Liu, Qi-Xing</au><au>Yang, Yu-Shun</au><au>Zhu, Hai-Liang</au><aucorp>aState Key Laboratory of Pharmaceutical Biotechnology</aucorp><aucorp>Linyi Central Hospital</aucorp><aucorp>Nanjing University</aucorp><aucorp>bCentral Laboratory</aucorp><format>journal</format><genre>article</genre><ristype>JOUR</ristype><atitle>Introducing Broadened Antibacterial Activity to Rhodanine Derivatives Targeting Enoyl-Acyl Carrier Protein Reductase</atitle><jtitle>Chemical & pharmaceutical bulletin</jtitle><addtitle>Chem. Pharm. Bull.</addtitle><date>2019-02-01</date><risdate>2019</risdate><volume>67</volume><issue>2</issue><spage>125</spage><epage>129</epage><pages>125-129</pages><issn>0009-2363</issn><eissn>1347-5223</eissn><abstract>Broadened antibacterial activity was introduced to rhodanine derivatives targeting Mycobacterial tuberculosis enoyl-acyl carrier protein reductase (Mtb InhA) by recruiting feature of xacins to bring DNA Gyrase B inhibitory capability. This is significant for preventing further bacterial injections in the tuberculosis treatment. The most potent compound Cy14 suggested comparable bioactivity (IC50 = 3.18 µM for Mtb InhA; IC50 = 10 nM for DNA Gyrase B) with positive controls. 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| source | J-STAGE Free; EZB-FREE-00999 freely available EZB journals; Free Full-Text Journals in Chemistry |
| subjects | Acyl carrier protein Antibacterial activity bacterial infection Biological activity computer assistant drug design Deoxyribonucleic acid Derivatives DNA DNA Gyrase B DNA topoisomerase enoyl-acyl carrier protein reductase Molecular docking Molecular structure Proteins Reductase rhodanine Tuberculosis |
| title | Introducing Broadened Antibacterial Activity to Rhodanine Derivatives Targeting Enoyl-Acyl Carrier Protein Reductase |
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