Bioorganic and Medicinal Chemistry Letters p. 1337 - 1342 (1997)
Update date:2022-09-26
Topics:
Semple, Graeme
Ashworth, Doreen M.
Baker, Graham R.
Batt, Andrzej R.
Baxter, Andrew J.
Benzies, David W.M.
Elliot, Lucy H.
Evans, D. Michael
Franklin, Richard J.
Hudson, Peter
Jenkins, Paul D.
Pitt, Gary R.
Rooker, David P.
Sheppard, Andrew
Szelke, Michael
Yamamoto, Satoshi
Isomura, Yasuo
New potent, reversible inhibitors of recombinant human Interleukin-1 β-converting enzyme (ICE, caspase-1) with significantly reduced peptide character are described. The compounds were designed by incorporation of pyridone and pyrimidone heterocyclic replacements for the P2-P3 amino acids of the native substrate and were optimised by manipulation of peripheral alkyl and aryl substituents.
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