2. Academic Validation
  3. Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors

Novel pyrazinone mono-amides as potent and reversible caspase-3 inhibitors

  • Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80. doi: 10.1016/j.bmcl.2004.12.006.
Yongxin Han 1,  André Giroux,  John Colucci,  Christopher I Bayly,  Daniel J Mckay,  Sophie Roy,  Steve Xanthoudakis,  John Vaillancourt,  Dita M Rasper,  John Tam,  Paul Tawa,  Donald W Nicholson,  Robert J Zamboni
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Merck Frosst Centre for Therapeutic Research, Merck Frosst Canada & Co., PO Box 1005, Pointe-Claire-Dorval, Quebec, Canada H9R 4P8. yongxin_han@merck.com
PMID: 15686936 DOI: 10.1016/j.bmcl.2004.12.006
Abstract

The iterative process for the discovery of a series of pyrazinone mono-amides as potent, selective and reversible non-peptide Caspase-3 inhibitors (e.g., M826 and M867) is reported. These compounds display potent anti apoptotic activities in a number of cell based systems in vitro as well as in several animal models in vivo.

Figures
Products
  • Cat. No.
    Product Name
    Description
    Target
    Research Area
  • HY-155613
    Caspase-3 Inhibitor