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Bioorg Med Chem Lett. 2005 Feb 15;15(4):1173-80.

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

Author information

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

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.

PMID:
15686936
DOI:
10.1016/j.bmcl.2004.12.006
[Indexed for MEDLINE]

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