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.date.accessioned2014-04-04T07:09:01Z
dc.date.available2014-04-04T07:09:01Z
dc.date.copyright2013en_US
dc.date.issued2013
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.identifier.issn0947-6539en_US
dc.identifier.urihttp://hdl.handle.net/10220/19119
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.language.isoenen_US
dc.relation.ispartofseriesChemistry - a European journalen_US
dc.rights© 2013 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim.en_US
dc.subjectDRNTU::Engineering::Materials
dc.titleSynthesis and extended activity of triazole-containing macrocyclic protease inhibitorsen_US
dc.typeJournal Article
dc.contributor.schoolSchool of Materials Science and Engineeringen_US
dc.identifier.doihttp://dx.doi.org/10.1002/chem.201204260


Files in this item

FilesSizeFormatView

There are no files associated with this item.

This item appears in the following Collection(s)

Show simple item record