2. Academic Validation
  3. Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors

Design, synthesis and antiviral efficacy of a series of potent chloropyridyl ester-derived SARS-CoV 3CLpro inhibitors

  • Bioorg Med Chem Lett. 2008 Oct 15;18(20):5684-8. doi: 10.1016/j.bmcl.2008.08.082.
Arun K Ghosh 1,  Gangli Gong,  Valerie Grum-Tokars,  Debbie C Mulhearn,  Susan C Baker,  Melissa Coughlin,  Bellur S Prabhakar,  Katrina Sleeman,  Michael E Johnson,  Andrew D Mesecar
Affiliations

Affiliation

  • 1 Department of Chemistry, Purdue University, 560 Oval drive, West Lafayette, IN 47907, USA. akghosh@purdue.edu
PMID: 18796354 DOI: 10.1016/j.bmcl.2008.08.082
Abstract

Design, synthesis and biological evaluation of a series of 5-chloropyridine ester-derived severe acute respiratory syndrome-coronavirus chymotrypsin-like Protease Inhibitors is described. Position of the carboxylate functionality is critical to potency. Inhibitor 10 with a 5-chloropyridinyl ester at position 4 of the indole ring is the most potent inhibitor with a SARS-CoV 3CLpro IC(50) value of 30 nM and an Antiviral EC(50) value of 6.9 microM. Molecular docking studies have provided possible binding modes of these inhibitors.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-137954
    99.20%, SARS-CoV 3CLpro Inhibitor