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Protein & Peptide Letters

Editor-in-Chief

ISSN (Print): 0929-8665
ISSN (Online): 1875-5305

N-Heterocyclic Dipeptide Aldehyde Calpain Inhibitors

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

Volume 16 , Issue 12 , 2009

Page: [1466 - 1472] Pages: 7

DOI: 10.2174/092986609789839296

Price: $65

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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