Synthesis and evaluation of azapeptide-derived inhibitors of serine and cysteine proteases

Todd L. Graybill, Mitchell J. Ross, Bruce R. Gauvin, Jill S. Gregory, Alex L. Harris, Mark A. Ator, James M. Rinker, Roland E. Dolle

Research output: Contribution to journalArticlepeer-review

54 Scopus citations

Abstract

Azapeptide analogues ii of the α-halomethyl ketones i were synthesized and evaluated as potential inhibitors of serine and cysteine proteases. Inhibitors ii discriminate between the two classes of protease, demonstrating selectivity for cysteine proteases. Azaglycines 1-3 and 5 displayed time-dependent inactivation (kobs/[I] = 200-1500 M-1s-1) of cathepsin B and calpain.

Original languageEnglish
Pages (from-to)1375-1380
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume2
Issue number11
DOIs
StatePublished - Nov 1992

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