N-heterocyclic dipeptide aldehyde calpain inhibitors

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dc.contributor.authorJones, S.
dc.contributor.authorJones, M.
dc.contributor.authorMcNabb, S.
dc.contributor.authorAitken, S.
dc.contributor.authorCoxon, J.
dc.contributor.authorAbell, A.
dc.date.issued2009
dc.description.abstractA 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.
dc.description.statementofresponsibilityJones, Seth A.; Jones, Matthew A.; McNabb, Stephen B.; Aitken, Steven G.; Coxon, James M. And Abell, Andrew D
dc.identifier.citationProtein and Peptide Letters: international journal for rapid publication of short papers in protein and peptide science, 2009; 16(12):1466-1472
dc.identifier.doi10.2174/092986609789839296
dc.identifier.issn0929-8665
dc.identifier.issn1875-5305
dc.identifier.orcidAbell, A. [0000-0002-0604-2629]
dc.identifier.urihttp://hdl.handle.net/2440/58623
dc.language.isoen
dc.publisherBentham Science Publ Ltd
dc.relation.grantARC
dc.source.urihttps://doi.org/10.2174/092986609789839296
dc.subjectCalpain inhibitors
dc.subjectpeptidic aldehydes
dc.subjectsynthesis
dc.subjectheterocycles
dc.titleN-heterocyclic dipeptide aldehyde calpain inhibitors
dc.typeJournal article
pubs.publication-statusPublished

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