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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Detalles Bibliográficos
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
Descripción
Sumario: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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