Author/Authors :
Todd L. Graybill، نويسنده , , Catherine P. Prouty، نويسنده , , Gary J. Speier، نويسنده , , Denton Hoyer، نويسنده , , Roland E. Dolle، نويسنده , , Carla T. Helaszek، نويسنده , , Mark A. Ator، نويسنده , , Joanne Uhl، نويسنده , , Joost Strastes، نويسنده ,
Abstract :
Aryl-substituted tetronic acids, tetramic acids, and cyclic β-dicarbonyl moieties were evaluated as leaving groups in the peptidyl-COCH2-X type inhibitor iii. Tripeptidyl aspartyl α-((tetronoyl)oxy)- and α-((tetramoyl)oxy)methyl ketone derivatives demonstrate potent time-dependent inhibition (kobs/[I] 100,000–250,000 M−1s−1) of the cysteine protease ICE.