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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Detalles Bibliográficos
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
Descripción
Sumario: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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