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Peptidomimetic aminomethylene ketone inhibitors of interleukin-1 beta-converting enzyme (ICE)
G Semple1, D M Ashworth, A R Batt
1Department of Medicinal Chemistry, Ferring Research Institute, Chilworth Research Centre, Southampton, U.K.
Bioorganic & Medicinal Chemistry Letters
|January 1, 1999
Abstract:
Pyridone-based peptidomimetic inhibitors of recombinant human Interleukin-1 beta-converting enzyme (ICE, caspase-1) with an aminomethylene ketone activating group in the P1' position are described. Several analogues with sub-nanomolar Ki's versus ICE and improved aqueous solubility are reported.