Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease
Identifieur interne : 000724 ( Pmc/Checkpoint ); précédent : 000723; suivant : 000725Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease
Auteurs : Hiroyuki Konno [Japon] ; Masaki Wakabayashi [Japon] ; Daiki Takanuma [Japon] ; Yota Saito [Japon] ; Kenichi Akaji [Japon]Source :
- Bioorganic & Medicinal Chemistry [ 0968-0896 ] ; 2016.
Abstract
Url:
DOI: 10.1016/j.bmc.2016.01.052
PubMed: 26879854
PubMed Central: 7111485
Affiliations:
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id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Takanuma, Daiki" sort="Takanuma, Daiki" uniqKey="Takanuma D" first="Daiki" last="Takanuma">Daiki Takanuma</name><affiliation wicri:level="1"><nlm:aff id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Saito, Yota" sort="Saito, Yota" uniqKey="Saito Y" first="Yota" last="Saito">Yota Saito</name><affiliation wicri:level="1"><nlm:aff id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Akaji, Kenichi" sort="Akaji, Kenichi" uniqKey="Akaji K" first="Kenichi" last="Akaji">Kenichi Akaji</name><affiliation wicri:level="1"><nlm:aff id="af010">Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of 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type="main">Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease</title><author><name sortKey="Konno, Hiroyuki" sort="Konno, Hiroyuki" uniqKey="Konno H" first="Hiroyuki" last="Konno">Hiroyuki Konno</name><affiliation wicri:level="1"><nlm:aff id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Wakabayashi, Masaki" sort="Wakabayashi, Masaki" uniqKey="Wakabayashi M" first="Masaki" last="Wakabayashi">Masaki Wakabayashi</name><affiliation wicri:level="1"><nlm:aff id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Takanuma, Daiki" sort="Takanuma, Daiki" uniqKey="Takanuma D" first="Daiki" last="Takanuma">Daiki Takanuma</name><affiliation wicri:level="1"><nlm:aff id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Saito, Yota" sort="Saito, Yota" uniqKey="Saito Y" first="Yota" last="Saito">Yota Saito</name><affiliation wicri:level="1"><nlm:aff id="af005">Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510</wicri:regionArea><wicri:noRegion>Yamagata 992-8510</wicri:noRegion></affiliation></author><author><name sortKey="Akaji, Kenichi" sort="Akaji, Kenichi" uniqKey="Akaji K" first="Kenichi" last="Akaji">Kenichi Akaji</name><affiliation wicri:level="1"><nlm:aff id="af010">Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan</nlm:aff><country xml:lang="fr">Japon</country><wicri:regionArea>Department of Medicinal Chemistry, Kyoto Pharmaceutical University, 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<front><journal-meta><journal-id journal-id-type="nlm-ta">Bioorg Med Chem</journal-id><journal-id journal-id-type="iso-abbrev">Bioorg. Med. Chem</journal-id><journal-title-group><journal-title>Bioorganic & Medicinal Chemistry</journal-title></journal-title-group><issn pub-type="ppub">0968-0896</issn><issn pub-type="epub">1464-3391</issn><publisher><publisher-name>Elsevier Ltd.</publisher-name></publisher></journal-meta><article-meta><article-id pub-id-type="pmid">26879854</article-id><article-id pub-id-type="pmc">7111485</article-id><article-id pub-id-type="publisher-id">S0968-0896(16)30066-9</article-id><article-id pub-id-type="doi">10.1016/j.bmc.2016.01.052</article-id><article-categories><subj-group subj-group-type="heading"><subject>Article</subject></subj-group></article-categories><title-group><article-title>Design and synthesis of a series of serine derivatives as small molecule inhibitors of the SARS coronavirus 3CL protease</article-title></title-group><contrib-group><contrib contrib-type="author" id="au005"><name><surname>Konno</surname><given-names>Hiroyuki</given-names></name><email>konno@yz.yamagata-u.ac.jp</email><xref rid="af005" ref-type="aff">a</xref><xref rid="cor1" ref-type="corresp">⁎</xref></contrib><contrib contrib-type="author" id="au010"><name><surname>Wakabayashi</surname><given-names>Masaki</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au015"><name><surname>Takanuma</surname><given-names>Daiki</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au020"><name><surname>Saito</surname><given-names>Yota</given-names></name><xref rid="af005" ref-type="aff">a</xref></contrib><contrib contrib-type="author" id="au025"><name><surname>Akaji</surname><given-names>Kenichi</given-names></name><email>akaji@mb.kyoto-phu.ac.jp</email><xref rid="af010" ref-type="aff">b</xref><xref rid="cor1" ref-type="corresp">⁎</xref></contrib></contrib-group><aff id="af005"><label>a</label>Department of Biological Engineering, Graduate School of Science and Technology, Yamagata University, Yonezawa, Yamagata 992-8510, Japan</aff><aff id="af010"><label>b</label>Department of Medicinal Chemistry, Kyoto Pharmaceutical University, Yamashina-ku, Kyoto 607-8414, Japan</aff><author-notes><corresp id="cor1"><label>⁎</label>Corresponding authors. Tel./fax: +81 (0)238 26 3131 (H.K.). <email>konno@yz.yamagata-u.ac.jp</email><email>akaji@mb.kyoto-phu.ac.jp</email></corresp></author-notes><pub-date pub-type="pmc-release"><day>29</day><month>1</month><year>2016</year></pub-date><pmc-comment> PMC Release delay is 0 months and 0 days and was based on .</pmc-comment>
<pub-date pub-type="ppub"><day>15</day><month>3</month><year>2016</year></pub-date><pub-date pub-type="epub"><day>29</day><month>1</month><year>2016</year></pub-date><volume>24</volume><issue>6</issue><fpage>1241</fpage><lpage>1254</lpage><history><date date-type="received"><day>13</day><month>1</month><year>2016</year></date><date date-type="rev-recd"><day>26</day><month>1</month><year>2016</year></date><date date-type="accepted"><day>27</day><month>1</month><year>2016</year></date></history><permissions><copyright-statement>Copyright © 2016 Elsevier Ltd. All rights reserved.</copyright-statement><copyright-year>2016</copyright-year><copyright-holder>Elsevier Ltd</copyright-holder><license><license-p>Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.</license-p></license></permissions><abstract abstract-type="graphical" id="ab005"><title>Graphical abstract</title><fig id="f0040" position="anchor"><graphic xlink:href="fx1_lrg"></graphic></fig></abstract><abstract id="ab010"><p>Synthesis of serine derivatives having the essential functional groups for the inhibitor of SARS 3CL protease and evaluation of their inhibitory activities using SARS 3CL R188I mutant protease are described. The lead compounds, functionalized serine derivatives, were designed based on the tetrapeptide aldehyde and Bai’s cinnamoly inhibitor, and additionally performed with simulation on GOLD softwear. Structure activity relationship studies of the candidate compounds were given reasonable inhibitors ent-<bold>3</bold> and ent-<bold>7k</bold> against SARS 3CL R188I mutant protease. These inhibitors showed protease selectivity and no cytotoxicity.</p></abstract><kwd-group id="kg005"><title>Keywords</title><kwd>SARS CoV</kwd><kwd>SARS 3CL protease</kwd><kwd>Serine derivative</kwd><kwd>Docking simulation</kwd><kwd>Cathepsin B</kwd><kwd>Cytotoxicity</kwd></kwd-group></article-meta></front></pmc><affiliations><list><country><li>Japon</li></country></list><tree><country name="Japon"><noRegion><name sortKey="Konno, Hiroyuki" sort="Konno, Hiroyuki" uniqKey="Konno H" first="Hiroyuki" last="Konno">Hiroyuki Konno</name></noRegion><name sortKey="Akaji, Kenichi" sort="Akaji, Kenichi" uniqKey="Akaji K" first="Kenichi" last="Akaji">Kenichi Akaji</name><name sortKey="Saito, Yota" sort="Saito, Yota" uniqKey="Saito Y" first="Yota" last="Saito">Yota Saito</name><name sortKey="Takanuma, Daiki" sort="Takanuma, Daiki" uniqKey="Takanuma D" first="Daiki" last="Takanuma">Daiki Takanuma</name><name sortKey="Wakabayashi, Masaki" sort="Wakabayashi, Masaki" uniqKey="Wakabayashi M" first="Masaki" last="Wakabayashi">Masaki Wakabayashi</name></country></tree></affiliations></record>Pour manipuler ce document sous Unix (Dilib)
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