Abstract
A novel diazocan containing dipeptide mimetic was synthesized via reductive N-N bond cleavage of a pyrazolidino-pyrazolidine using Raney-Ni and evaluated as an ICE inhibitor. This versatile 8-membered ring containing scaffold possesses an N-5 ring nitrogen that was used to explore structure-activity relationships in a cell-based assay measuring inhibition of interleukin-1beta.
MeSH terms
-
Caspase Inhibitors
-
Dipeptides / chemical synthesis*
-
Dipeptides / chemistry
-
Dipeptides / pharmacology
-
Drug Evaluation, Preclinical
-
Inhibitory Concentration 50
-
Interleukin-1 / antagonists & inhibitors*
-
Interleukin-1 / biosynthesis
-
Molecular Conformation
-
Molecular Mimicry
-
Peptides, Cyclic / chemical synthesis*
-
Peptides, Cyclic / chemistry
-
Peptides, Cyclic / pharmacology
-
Pyrazoles / chemistry
-
Structure-Activity Relationship
Substances
-
Caspase Inhibitors
-
Dipeptides
-
Interleukin-1
-
Peptides, Cyclic
-
Pyrazoles
-
diazocan