Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus

The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nan...

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Autores principales: Mandadapu, Sivakoteswara Rao, Weerawarna, Pathum M., Prior, Allan M., Uy, Roxanne Adeline Z., Aravapalli, Sridhar, Alliston, Kevin R., Lushington, Gerald H., Kim, Yunjeong, Hua, Duy H., Chang, Kyeong-Ok, Groutas, William C.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2013
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3750990/
https://www.ncbi.nlm.nih.gov/pubmed/23727045
http://dx.doi.org/10.1016/j.bmcl.2013.05.021
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author Mandadapu, Sivakoteswara Rao
Weerawarna, Pathum M.
Prior, Allan M.
Uy, Roxanne Adeline Z.
Aravapalli, Sridhar
Alliston, Kevin R.
Lushington, Gerald H.
Kim, Yunjeong
Hua, Duy H.
Chang, Kyeong-Ok
Groutas, William C.
author_facet Mandadapu, Sivakoteswara Rao
Weerawarna, Pathum M.
Prior, Allan M.
Uy, Roxanne Adeline Z.
Aravapalli, Sridhar
Alliston, Kevin R.
Lushington, Gerald H.
Kim, Yunjeong
Hua, Duy H.
Chang, Kyeong-Ok
Groutas, William C.
author_sort Mandadapu, Sivakoteswara Rao
collection PubMed
description The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nancy strain), and coronavirus (SARS-CoV) and norovirus 3C-like proteases, was determined to be 1.8, 15.5 and 5.1 μM, respectively.
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spelling pubmed-37509902014-07-01 Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus Mandadapu, Sivakoteswara Rao Weerawarna, Pathum M. Prior, Allan M. Uy, Roxanne Adeline Z. Aravapalli, Sridhar Alliston, Kevin R. Lushington, Gerald H. Kim, Yunjeong Hua, Duy H. Chang, Kyeong-Ok Groutas, William C. Bioorg Med Chem Lett Article The design, synthesis, and in vitro evaluation of the first macrocyclic inhibitor of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus are reported. The in vitro inhibitory activity (50% effective concentration) of the macrocyclic inhibitor toward enterovirus 3C protease (CVB3 Nancy strain), and coronavirus (SARS-CoV) and norovirus 3C-like proteases, was determined to be 1.8, 15.5 and 5.1 μM, respectively. Elsevier Ltd. 2013-07-01 2013-05-16 /pmc/articles/PMC3750990/ /pubmed/23727045 http://dx.doi.org/10.1016/j.bmcl.2013.05.021 Text en Copyright © 2013 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
Mandadapu, Sivakoteswara Rao
Weerawarna, Pathum M.
Prior, Allan M.
Uy, Roxanne Adeline Z.
Aravapalli, Sridhar
Alliston, Kevin R.
Lushington, Gerald H.
Kim, Yunjeong
Hua, Duy H.
Chang, Kyeong-Ok
Groutas, William C.
Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus
title Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus
title_full Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus
title_fullStr Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus
title_full_unstemmed Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus
title_short Macrocyclic inhibitors of 3C and 3C-like proteases of picornavirus, norovirus, and coronavirus
title_sort macrocyclic inhibitors of 3c and 3c-like proteases of picornavirus, norovirus, and coronavirus
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3750990/
https://www.ncbi.nlm.nih.gov/pubmed/23727045
http://dx.doi.org/10.1016/j.bmcl.2013.05.021
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