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Molecular Modeling,Synthesis, and Biological Evaluation of Macrocyclic Calpain Inhibitors |
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| Authors: | Andrew D Abell Prof Matthew A Jones Dr James M Coxon Prof James D Morton Dr Steven G Aitken Dr Stephen B McNabb Dr Hannah Y‐Y Lee Dr Janna M Mehrtens Dr Nathan A Alexander Dr Blair G Stuart Axel T Neffe Dr Roy Bickerstaffe Prof |
| Institution: | 1. Department of Chemistry, University of Canterbury, Private Bag 4800, Christchurch (New Zealand);2. Present address: School of Chemistry & Physics, The University of Adelaide, North Terrace, Adelaide, SA 5005 (Australia), Fax: (+61)?8‐8303‐4358;3. Agriculture and Life Sciences Division, Lincoln University, Post Office Box 84, Canterbury (New Zealand), Fax: (+64)?3‐325‐3851;4. Present address: Institute of Polymer Research, GKSS Research, Centre Geesthacht GmbH, Kantstrasse 55, 14513 Teltow (Germany) |
| Abstract: | 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.  |
| Keywords: | biological activity inhibitors macrocycles molecular modeling peptides |