Molecular Modeling, Synthesis, and Biological Evaluation of Macrocyclic Calpain Inhibitors

The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a β-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacification in an ovine-lens culture assay and is a lead compo...

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Veröffentlicht in:Angewandte Chemie (International ed.) 2009-01, Vol.48 (8), p.1455-1458
Hauptverfasser: Abell, Andrew D, Jones, Matthew A, Coxon, James M, Morton, James D, Aitken, Steven G, McNabb, Stephen B, Lee, Hannah Y.-Y, Mehrtens, Janna M, Alexander, Nathan A, Stuart, Blair G, Neffe, Axel T, Bickerstaffe, Roy
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Sprache:eng
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Zusammenfassung:The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a β-strand-like peptide-backbone conformation led to potent and selective inhibitors of calpain 2. Macrocycle 1 retarded calcium-induced opacification in an ovine-lens culture assay and is a lead compound for the development of a drug for cataract treatment. Cbz=carbobenzyloxy.
ISSN:1433-7851
1521-3773
DOI:10.1002/anie.200805014