Synthesis and evaluation of novel 8,6-fused bicyclic peptidomimetic compounds as interleukin-1b converting enzyme inhibitors

Procter & Gamble Pharmaceuticals, Inc., 8700 Mason-Montgomery Road, Mason, OH 45040, USA.
Bioorganic & Medicinal Chemistry Letters (Impact Factor: 2.42). 01/2006; 15(24):5434-8. DOI: 10.1016/j.bmcl.2005.08.109
Source: PubMed


Two novel 8,6-fused bicyclic peptidomimetic ring systems were synthesized utilizing olefin metathesis as the key reaction for the formation of the eight-membered ring. Both peptidomimetic scaffolds were further elaborated into potent ICE inhibitors, with numerous compounds exhibiting caspase-1 IC(50)s less than 10nM.

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