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

被引:33
|
作者
Semple, G
Ashworth, DM
Baker, GR
Batt, AR
Baxter, AJ
Benzies, DWM
Elliot, LH
Evans, DM
Franklin, RJ
Hudson, P
Jenkins, PD
Pitt, GR
Rooker, DP
Sheppard, A
Szelke, M
Yamamoto, S
Isomura, Y
机构
[1] CHILWORTH RES CTR,FERRING RES INST,DEPT BIOL,SOUTHAMPTON SO16 7NP,HANTS,ENGLAND
[2] YAMANOUCHI INST DRUG DISCOVERY RES,INFECT DIS & IMMUNOL RES LABS,TSUKUBA,IBARAKI 305,JAPAN
关键词
D O I
10.1016/S0960-894X(97)00220-5
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
New potent, reversible inhibitors of recombinant human Interleukin-1 beta-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 P-2-P-3 amino acids of the native substrate and were optimised by manipulation of peripheral alkyl and aryl substituents. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:1337 / 1342
页数:6
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