N-Heterocyclic Dipeptide Aldehyde Calpain Inhibitors

Author(s): Seth A. Jones, Matthew A. Jones, Stephen B. McNabb, Steven G. Aitken, James M. Coxon, Andrew D. Abell.

Journal Name: Protein & Peptide Letters

Volume 16 , Issue 12 , 2009

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Abstract:

A series of Val-Leu based peptidic aldehydes containing either a furan or thiophene at the Nterminus 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.

Keywords: Calpain inhibitors, peptidic aldehydes, synthesis, heterocycles

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Article Details

VOLUME: 16
ISSUE: 12
Year: 2009
Page: [1466 - 1472]
Pages: 7
DOI: 10.2174/092986609789839296
Price: $58

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