Succinic acid amides as P2-P3 replacements for inhibitors of interleukin-1beta converting enzyme (ICE or caspase 1).
Bioorg Med Chem Lett
; 20(17): 5184-90, 2010 Sep 01.
Article
in En
| MEDLINE
| ID: mdl-20656488
ABSTRACT
Succinic acid amides have been found to be effective P2-P3 scaffold replacements for peptidic ICE inhibitors. Heteroarylalkyl fragments occupying the P4 position provided access to compounds with nM affinities. Utilization of an acylal prodrug moiety was required to overcome biopharmaceutical issues which led to the identification of 17f, a potential clinical candidate.
Full text:
1
Collection:
01-internacional
Database:
MEDLINE
Main subject:
Cysteine Proteinase Inhibitors
/
Succinic Acid
/
Caspase Inhibitors
/
Amides
Language:
En
Journal:
Bioorg Med Chem Lett
Journal subject:
BIOQUIMICA
/
QUIMICA
Year:
2010
Document type:
Article
Affiliation country:
United States
Country of publication:
ENGLAND
/
ESCOCIA
/
GB
/
GREAT BRITAIN
/
INGLATERRA
/
REINO UNIDO
/
SCOTLAND
/
UK
/
UNITED KINGDOM