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
Protein & Peptide Letters
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.
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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
DOI https://dx.doi.org/10.2174/092986609789839296 |
Print ISSN 0929-8665 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-5305 |
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