Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor

Synthesis and evaluation of new scaffold phenylisoserine derivatives connected with the essential functional groups against SARS CoV 3CL protease are described. The phenylisoserine backbone was found by simulation on GOLD software and the structure activity relationship study of phenylisoserine deri...

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Autores principales: Konno, Hiroyuki, Onuma, Takumi, Nitanai, Ikumi, Wakabayashi, Masaki, Yano, Shigekazu, Teruya, Kenta, Akaji, Kenichi
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2017
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127027/
https://www.ncbi.nlm.nih.gov/pubmed/28454669
http://dx.doi.org/10.1016/j.bmcl.2017.04.056
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author Konno, Hiroyuki
Onuma, Takumi
Nitanai, Ikumi
Wakabayashi, Masaki
Yano, Shigekazu
Teruya, Kenta
Akaji, Kenichi
author_facet Konno, Hiroyuki
Onuma, Takumi
Nitanai, Ikumi
Wakabayashi, Masaki
Yano, Shigekazu
Teruya, Kenta
Akaji, Kenichi
author_sort Konno, Hiroyuki
collection PubMed
description Synthesis and evaluation of new scaffold phenylisoserine derivatives connected with the essential functional groups against SARS CoV 3CL protease are described. The phenylisoserine backbone was found by simulation on GOLD software and the structure activity relationship study of phenylisoserine derivatives gave SK80 with an IC(50) value of 43 μM against SARS CoV 3CL R188I mutant protease.
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spelling pubmed-71270272020-04-08 Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor Konno, Hiroyuki Onuma, Takumi Nitanai, Ikumi Wakabayashi, Masaki Yano, Shigekazu Teruya, Kenta Akaji, Kenichi Bioorg Med Chem Lett Article Synthesis and evaluation of new scaffold phenylisoserine derivatives connected with the essential functional groups against SARS CoV 3CL protease are described. The phenylisoserine backbone was found by simulation on GOLD software and the structure activity relationship study of phenylisoserine derivatives gave SK80 with an IC(50) value of 43 μM against SARS CoV 3CL R188I mutant protease. Elsevier Ltd. 2017-06-15 2017-04-20 /pmc/articles/PMC7127027/ /pubmed/28454669 http://dx.doi.org/10.1016/j.bmcl.2017.04.056 Text en © 2017 Elsevier Ltd. All rights reserved. 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.
spellingShingle Article
Konno, Hiroyuki
Onuma, Takumi
Nitanai, Ikumi
Wakabayashi, Masaki
Yano, Shigekazu
Teruya, Kenta
Akaji, Kenichi
Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
title Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
title_full Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
title_fullStr Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
title_full_unstemmed Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
title_short Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor
title_sort synthesis and evaluation of phenylisoserine derivatives for the sars-cov 3cl protease inhibitor
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7127027/
https://www.ncbi.nlm.nih.gov/pubmed/28454669
http://dx.doi.org/10.1016/j.bmcl.2017.04.056
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