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

Hiroyuki Konno, Takumi Onuma, Ikumi Nitanai, Masaki Wakabayashi, Shigekazu Yano, Kenta Teruya, Kenichi Akaji

Research output: Contribution to journalArticlepeer-review

17 Citations (Scopus)

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 43 μM against SARS CoV 3CL R188I mutant protease.

Original languageEnglish
Pages (from-to)2746-2751
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number12
DOIs
Publication statusPublished - 2017
Externally publishedYes

Keywords

  • Cinnamoyl
  • Docking simulation
  • Phenylisoserine derivative
  • SARS 3CL protease
  • SARS CoV

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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