Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1β synthesis

A novel diazocan containing dipeptide mimetic was synthesized via reductive N–N bond cleavage of a pyrazolidino-pyrazolidine using Raney-Ni and evaluated as an ICE inhibitor. This versatile 8-membered ring containing scaffold possesses an N-5 ring nitrogen that was used to explore structure-activity relationships in a cell-based assay measuring inhibition of interleukin-1β.

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