Synthesis and evaluation of diacylhydrazines as inhibitors of the interleukin-1β converting enzyme (ICE)

Todd L. Graybill, Roland E. Dolle, Carla T. Helaszek, Mark A. Ator, Joost Strasters

Research output: Contribution to journalArticlepeer-review

13 Scopus citations

Abstract

Diacylhydrazines ([azaAsp1] derivatives) were prepared and shown to inactivate ICE in a time-dependent manner. Inactivation rates for most of these diacylhydrazines were 10-fold slower than their α-substituted methylketone congeners. Rates for 6 and 7 (ca. 18,000 M-1s-1) compared favorably to those reported for Ac-Tyr-Val-Ala-Asp-CH-N2 and azapeptide inhibitors for other cysteine proteases.

Original languageEnglish
Pages (from-to)1197-1202
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume5
Issue number11
DOIs
StatePublished - Jun 8 1995

Fingerprint

Dive into the research topics of 'Synthesis and evaluation of diacylhydrazines as inhibitors of the interleukin-1β converting enzyme (ICE)'. Together they form a unique fingerprint.

Cite this