dc.contributor.authorPehere, Ashok D.
dc.contributor.authorPietsch, Markus
dc.contributor.authorGütschow, Michael
dc.contributor.authorNeilsen, Paul M.
dc.contributor.authorPedersen, Daniel Sejer
dc.contributor.authorNguyen, Steven
dc.contributor.authorZvarec, Ondrej
dc.contributor.authorSykes, Matthew J.
dc.contributor.authorCallen, David F.
dc.contributor.authorAbell, Andrew D.
dc.identifier.citationPehere, A. D., Pietsch, M., Gütschow, M., Neilsen, P. M., Pedersen, D. S., Nguyen, S., et al. (2013). Synthesis and extended activity of triazole-containing macrocyclic protease inhibitors. Chemistry - A European Journal, 19(24), 7975-7981.en_US
dc.description.abstractPeptide-derived protease inhibitors are an important class of compounds with the potential to treat a wide range of diseases. Herein, we describe the synthesis of a series of triazole-containing macrocyclic protease inhibitors pre-organized into a β-strand conformation and an evaluation of their activity against a panel of proteases. Acyclic azido–alkyne-based aldehydes are also evaluated for comparison. The macrocyclic peptidomimetics showed considerable activity towards calpain II, cathepsin L and S, and the 20S proteasome chymotrypsin-like activity. Some of the first examples of highly potent macrocyclic inhibitors of cathepsin S were identified. These adopt a well-defined β-strand geometry as shown by NMR spectroscopy, X-ray analysis, and molecular docking studies.en_US
dc.relation.ispartofseriesChemistry - a European journalen_US
dc.rights© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.en_US
dc.titleSynthesis and extended activity of triazole-containing macrocyclic protease inhibitorsen_US
dc.typeJournal Article
dc.contributor.schoolSchool of Materials Science and Engineeringen_US

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