Molecular Modeling, Synthesis, and Biological Evaluation of Macrocyclic Calpain Inhibitors
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 compo...
Gespeichert in:
Veröffentlicht in: | Angewandte Chemie (International ed.) 2009-01, Vol.48 (8), p.1455-1458 |
---|---|
Hauptverfasser: | , , , , , , , , , , , |
Format: | Artikel |
Sprache: | eng |
Schlagworte: | |
Online-Zugang: | Volltext |
Tags: |
Tag hinzufügen
Keine Tags, Fügen Sie den ersten Tag hinzu!
|
Zusammenfassung: | 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. |
---|---|
ISSN: | 1433-7851 1521-3773 |
DOI: | 10.1002/anie.200805014 |