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Molecular Modeling, Synthesis, and Biological Evaluation of Macrocyclic Calpain Inhibitors
Author(s) -
Abell Andrew D.,
Jones Matthew A.,
Coxon James M.,
Morton James D.,
Aitken Steven G.,
McNabb Stephen B.,
Lee Hannah Y.Y.,
Mehrtens Janna M.,
Alexander Nathan A.,
Stuart Blair G.,
Neffe Axel T.,
Bickerstaffe Roy
Publication year - 2009
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.200805014
Subject(s) - calpain , chemistry , template , combinatorial chemistry , stereochemistry , molecular model , peptide , lens (geology) , biochemistry , biophysics , nanotechnology , biology , enzyme , materials science , paleontology
The design and elaboration of a series of macrocyclic templates that exhibit a propensity to adopt a β‐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.