New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors

Bioorg Med Chem Lett. 2009 May 15;19(10):2722-7. doi: 10.1016/j.bmcl.2009.03.118. Epub 2009 Mar 28.

Abstract

A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Three candidates had encouraging results for the development of new anti-SARS compounds.

Publication types

  • Research Support, N.I.H., Extramural
  • Research Support, Non-U.S. Gov't

MeSH terms

  • Amino Acid Sequence
  • Antiviral Agents / chemical synthesis*
  • Antiviral Agents / chemistry
  • Antiviral Agents / pharmacology
  • Benzothiazoles / chemical synthesis
  • Benzothiazoles / chemistry
  • Benzothiazoles / pharmacology
  • Chymases / antagonists & inhibitors
  • Chymases / metabolism
  • Computer Simulation
  • Coronavirus 3C Proteases
  • Cysteine Endopeptidases / metabolism
  • Drug Design
  • Ketones / chemical synthesis
  • Ketones / chemistry
  • Peptides / chemical synthesis
  • Peptides / chemistry
  • Peptides / pharmacology
  • Protease Inhibitors / chemical synthesis*
  • Protease Inhibitors / chemistry
  • Protease Inhibitors / pharmacology
  • Pyrrolidinones / chemical synthesis
  • Pyrrolidinones / chemistry
  • Pyrrolidinones / pharmacology
  • Severe acute respiratory syndrome-related coronavirus*
  • Structure-Activity Relationship
  • Thiazoles / chemical synthesis
  • Thiazoles / chemistry
  • Thiazoles / pharmacology
  • Viral Proteins / antagonists & inhibitors*
  • Viral Proteins / metabolism

Substances

  • Antiviral Agents
  • Benzothiazoles
  • Ketones
  • Peptides
  • Protease Inhibitors
  • Pyrrolidinones
  • Thiazoles
  • Viral Proteins
  • Chymases
  • Cysteine Endopeptidases
  • Coronavirus 3C Proteases