N-Heterocyclic Dipeptide Aldehyde Calpain Inhibitors

Title: N-Heterocyclic Dipeptide Aldehyde Calpain Inhibitors

Volume: 16 Issue: 12

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

Affiliation:

Keywords: Calpain inhibitors, peptidic aldehydes, synthesis, heterocycles

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.

Cite this article as:

Jones A. Seth, Jones A. Matthew, McNabb B. Stephen, Aitken G. Steven, Coxon M. James and Abell D. Andrew, N-Heterocyclic Dipeptide Aldehyde Calpain Inhibitors, Protein & Peptide Letters 2009; 16 (12) . https://dx.doi.org/10.2174/092986609789839296