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.
|Number of pages||6|
|Journal||Bioorganic and Medicinal Chemistry Letters|
|State||Published - Nov 1992|