Pyridone-based peptidomimetic inhibitors of interleukin-1β-converting enzyme (ICE)

…, DM Evans, RJ Franklin, P Hudson, PD Jenkins…

文献索引：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 Bioorganic and Medicinal Chemistry Letters, 1997 , vol. 7, # 10 p. 1337 - 1342

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被引用次数: 29

摘要

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.