Adelaide Research & Scholarship
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https://hdl.handle.net/2440/55162
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| Type: | Journal article |
| Title: | Molecular modeling, synthesis, and biological evaluation of macrocyclic calpain inhibitors |
| Author: | Abell, A. Jones, M. Coxon, J. Morton, J. Aitken, S. McNabb, S. Lee, H. Mehrtens, J. Alexander, N. Stuart, B. Neffe, A. Bickerstaffe, R. |
| Citation: | Angewandte Chemie International Edition, 2009; 48(8):1455-1458 |
| Publisher: | Wiley-V C H Verlag GMBH |
| Issue Date: | 2009 |
| ISSN: | 1433-7851 1521-3773 |
| Statement of Responsibility: | 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 and Roy Bickerstaffe |
| 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. |
| Keywords: | biological activity inhibitors macrocycles molecular modeling peptides |
| DOI: | 10.1002/anie.200805014 |
| Grant ID: | ARC |
| Published version: | http://dx.doi.org/10.1002/anie.200805014 |
| Appears in Collections: | Aurora harvest Chemistry publications |
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