Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors.

Andrew D Abell, Matthew A Jones, James M Coxon, James D Morton, Steven G Aitken, Stephen B McNabb, Hannah Y-Y Lee, Janna M Mehrtens, Nathan A Alexander, Blair G Stuart, Axel T Neffe, Roy Bickerstaffe

Department of Chemistry, University of Canterbury, Private Bag 4800, Christchurch, New Zealand.

Angewandte Chemie (International ed. in English) 2009

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The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a beta-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.

Citation

Andrew D Abell, Matthew A Jones, James M Coxon, James D Morton, Steven G Aitken, Stephen B McNabb, Hannah Y-Y Lee, Janna M Mehrtens, Nathan A Alexander, Blair G Stuart, Axel T Neffe, Roy Bickerstaffe. Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors. Angewandte Chemie (International ed. in English). 2009;48(8):1455-8