α-((Tetronoyl)oxy)- and α-((tetramoyl)oxy)methyl ketone inhibitors of the interleukin-1β converting enzyme (ICE)

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

• Publisher: Elsevier Science
• Year: 1997
• Tongue: English
• Weight: 386 KB
• Volume: 7
• Category: Article
• ISSN: 0960-894X
• DOI: 10.1016/s0960-894x(96)00574-4

✦ Synopsis

Aryl-substituted tetronic acids, tetramic acids, and cyclic ~-dicarbonyl moieties were evaluated as leaving groups in the peptidyl-COCH2-X type inhibitor iii. Tripeptidyl aspartyl et-((tetronoyl)oxy)-and ~-((tetramoyl)oxy)methyl ketone derivatives demonstrate potent time-dependent inhibition (kob,/[I] 100,000-250,000 M-ts -~) of the cysteine protease ICE.