P3 SAR exploration of biphenyl carbamate based Legumain inhibitors

Higgins, C. et al. (2014) P3 SAR exploration of biphenyl carbamate based Legumain inhibitors. Bioorganic and Medicinal Chemistry Letters, 24(11), pp. 2521-2524. (doi: 10.1016/j.bmcl.2014.04.002)

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Publisher's URL: http://dx.doi.org/10.1016/j.bmcl.2014.04.002

Abstract

This Letter describes the further development and SAR exploration of a novel series of Legumain inhibitors. Based upon a previously identified Legumain inhibitor from our group, we explored the SAR of the carbamate phenyl ring system to probe the P3 pocket of the enzyme. This led to the identification of a sub-nanomolar inhibitor of Legumain.

Item Type:Articles
Status:Published
Refereed:Yes
Glasgow Author(s) Enlighten ID:Gaddale Devanna, Dr Kishore Kumar
Authors: Higgins, C., Bouazzaoui, S., Gaddale, K., D’Costa, Z., Templeman, A., O’Rourke, M., Young, A., Scott, C., Harrison, T., Mullan, P., and Williams, R.
College/School:College of Science and Engineering > School of Chemistry
Journal Name:Bioorganic and Medicinal Chemistry Letters
Publisher:Elsevier
ISSN:0960-894X
ISSN (Online):1464-3405

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