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  • Title: Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors.
    Author: Abell AD, Jones MA, Coxon JM, Morton JD, Aitken SG, McNabb SB, Lee HY, Mehrtens JM, Alexander NA, Stuart BG, Neffe AT, Bickerstaffe R.
    Journal: Angew Chem Int Ed Engl; 2009; 48(8):1455-8. PubMed ID: 19145612.
    Abstract:
    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.
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