N-heterocyclic dipeptide aldehyde calpain inhibitors
Seth A Jones1, Matthew A Jones, Stephen B McNabb
1School of Chemistry & Physics, University of Adelaide, North Terrace, Adelaide, SA 5005, Australia.
Protein and Peptide Letters
|December 17, 2009
Abstract:
A series of Val-Leu based peptidic aldehydes containing either a furan or thiophene at the N-terminus was prepared and assayed against ovine m-calpain. In general, potency is favoured by a 2-substituted (rather than 3-substituted) heterocycle, a thiophene rather than a furan, and a shorter chain length at the N-terminus. Molecular docking experiments provide some rationale for these observations.
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