1359969-05-3Relevant academic research and scientific papers
MACROCYCLIC COMPOUNDS AND USES THEREOF
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Paragraph 00262, (2014/06/11)
The present invention relates to novel macrocyclic compounds of Formula I and their use as novel therapeutic agents for example as novel compounds used in methods of preventing and/or treating a disease, condition or state in a subject associated with dysregulation of protease activity and/or dysregulation of proteosome activity
New β-strand templates constrained by Huisgen cycloaddition
Pehere, Ashok D.,Abell, Andrew D.
, p. 1330 - 1333 (2012/05/20)
New peptidic templates constrained into a β-strand geometry by linking acetylene and azide containing P1 and P3 residues of a tripeptide by Huisgen cycloaddition are presented. The conformations of the macrocycles are defined by NMR studies and those that best define a β-strand are shown to be potent inhibitors of the protease calpain. The β-strand templates presented and defined here are prepared under optimized conditions that should be suitable for targeting a range of proteases and other applications requiring such a geometry.
