PYRIDONE-BASED PEPTIDOMIMETIC INHIBITORS OF INTERLEUKIN-1β-CONVERTING ENZYME (ICE)

Authors :: Lucy H. Elliot
Pitt Gary Robert William
Franklin Richard Jeremy
Doreen M. Ashworth
Michael Szelke
Satoshi Yamamoto
Andrew John Baxter
Graham R. Baker
D.Michael Evans
Andrew Sheppard
David W.M. Benzies
Graeme Semple
Rooker David Philip
Peter Hudson
Paul D. Jenkins
Andrzej Roman Batt
Yasuo Isomura
Source :: Bioorganic & Medicinal Chemistry Letters. 7:1337-1342
Publication Year :: 1997
Publisher :: Elsevier BV, 1997.
Abstract: New potent, reversible inhibitors of recombinant human Interleukin-1β-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. © 1997 Elsevier Science Ltd.

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