TY - JOUR
T1 - α-((Tetronoyl)oxy)- and α-((tetramoyl)oxy)methyl ketone inhibitors of the interleukin-1β converting enzyme (ICE)
AU - Graybill, Todd L.
AU - Prouty, Catherine P.
AU - Speier, Gary J.
AU - Hoyer, Denton
AU - Dolle, Roland E.
AU - Helaszek, Carla T.
AU - Ator, Mark A.
AU - Uhl, Joanne
AU - Strasters, Joost
PY - 1997/1/7
Y1 - 1997/1/7
N2 - Aryl-substituted tetronic acids, tetramic acids, and cyclic P-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 (k(obs)/[I] 100,000-250,000 M-1 s-1) of the cysteine protease ICE.
AB - Aryl-substituted tetronic acids, tetramic acids, and cyclic P-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 (k(obs)/[I] 100,000-250,000 M-1 s-1) of the cysteine protease ICE.
UR - http://www.scopus.com/inward/record.url?scp=0031033587&partnerID=8YFLogxK
U2 - 10.1016/S0960-894X(96)00574-4
DO - 10.1016/S0960-894X(96)00574-4
M3 - Article
AN - SCOPUS:0031033587
SN - 0960-894X
VL - 7
SP - 41
EP - 46
JO - Bioorganic and Medicinal Chemistry Letters
JF - Bioorganic and Medicinal Chemistry Letters
IS - 1
ER -