RRC ID 71764
Author Konno H, Onuma T, Nitanai I, Wakabayashi M, Yano S, Teruya K, Akaji K.
Title Synthesis and evaluation of phenylisoserine derivatives for the SARS-CoV 3CL protease inhibitor.
Journal Bioorg Med Chem Lett
Abstract 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 IC50 value of 43μM against SARS CoV 3CL R188I mutant protease.
Volume 27(12)
Pages 2746-2751
Published 2017-6-15
DOI 10.1016/j.bmcl.2017.04.056
PII S0960-894X(17)30433-X
PMID 28454669
PMC PMC7127027
MeSH Coronavirus 3C Proteases Cysteine Endopeptidases / genetics Cysteine Endopeptidases / metabolism Dose-Response Relationship, Drug Humans Models, Molecular Molecular Structure Protease Inhibitors / chemical synthesis Protease Inhibitors / chemistry Protease Inhibitors / pharmacology* Serine / analogs & derivatives* Serine / chemical synthesis Serine / chemistry Serine / pharmacology Structure-Activity Relationship Viral Proteins / antagonists & inhibitors* Viral Proteins / genetics Viral Proteins / metabolism
IF 2.572
Resource
Human and Animal Cells HeLa(RCB0007)