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Bioorg Med Chem Lett. 2006 Mar 15;16(6):1586-9. Epub 2005 Dec 27.

Novel dual inhibitors of calpain and lipid peroxidation with enhanced cellular activity.

Author information

1
Department of Medicinal Chemistry, Ipsen Research Laboratories, Institut Henri Beaufour, 5 Avenue du Canada, 91966 Les Ulis Cedex, France. serge.auvin@ipsen.com

Abstract

A series of dipeptides with dual inhibitory activities on calpain and lipid peroxidation were prepared to target the intracellular calpain. This optimization program focused on the variations of the linker and the N-terminal amino acid of the peptidic core. Two compounds 6d-05 and 6d-08 exhibited potent intracellular calpain inhibition. The polar surface area and the number of rotors appeared to be critical descriptors to account for the behavior of these hybrid molecules in the cellular calpain assay.

PMID:
16380258
DOI:
10.1016/j.bmcl.2005.12.036
[Indexed for MEDLINE]

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