| abstract |
This invention provides caspase inhibitors of formula (I): wherein Z is oxygen or sulfur; R1 is hydrogen, -CHN¿2?,R, CH2OR, CH2SR, or -CH2Y; Y is an electronegative leaving group; R?2¿ is CO¿2?H, CH2CO2H, or esters, amides or isosteres thereof; R?3¿ is a group capable of fitting into the S2 subsite of a caspase enzyme; R?4 and R5¿ are taken together with the intervening nitrogen to form heterocyclic ring and R is as described in the specification. The compounds are effective inhibitors of apoptosis and IL-1β secretion. |