Semple G, Ashworth D M, Batt A R, Baxter A J, Benzies D W, Elliot L H, Evans D M, Franklin R J, Hudson P, Jenkins P D, Pitt G R, Rooker D P, Yamamoto S, Isomura Y
Department of Medicinal Chemistry, Ferring Research Institute, Chilworth Research Centre, Southampton, U.K.
Bioorg Med Chem Lett. 1998 Apr 21;8(8):959-64. doi: 10.1016/s0960-894x(98)00136-x.
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.
