Alpha-((Tetronoyl)Oxy)- And Alpha-((Tetramoyl)Oxy)Methyl Ketone Inhibitors Of The Interleukin-1 Beta Converting Enzyme (Ice)

Todd L. Graybill,Catherine P. Prouty,Gary J. Speier,Denton Hoyer,Roland E. Dolle,Carla T. Helaszek,Mark A. Ator,Joanne Uhl,Joost Strastes

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS（1997）

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摘要

Aryl-substituted tetronic acids, tetramic acids, and cyclic beta-dicarbonyl moieties were evaluated as leaving groups in the peptidyl-COCH2-X type inhibitor iii. Tripeptidyl aspartyl alpha-((tetronoyl)oxy)- and alpha-((tetramoyl)oxy)methyl ketone derivatives demonstrate potent time-dependent inhibition (k(obs)/[T] 100,000-250,000 M(-1)s(-1)) of the cysteine protease ICE. Copyright (C) 1996 Elsevier Science Ltd

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