New tripeptide-based macrocyclic calpain inhibitors formed by N-alkylation of histidine

• Main Authors: Chen, Hongyuan, Jiao, Wanting, Bickerstaffe, Roy, Zvarec, Ondrej, Jones, Matthew A., Coxon, James M., Morton, James D., Pehere, Ashok D., Abell, Andrew D.
• Other Authors: School of Materials Science & Engineering
• Format: Article
• Language: English
• Published: 2013
• Online Access: https://hdl.handle.net/10356/96707; http://hdl.handle.net/10220/13036
• Institution: Nanyang Technological University

Two new series of 15-membered macrocyclic peptidomimetics, in which the P1 and P3 residues of the peptide backbone are linked by a bridge containing a 1,4-disubstituted 1H-imidazole, are reported. The structure with an aldehyde at the C-terminus and the imidazole at P3, i.e., 4c, shows significant i...