2. Academic Validation
  3. Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis

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

  • Bioorg Med Chem Lett. 2005 Oct 1;15(19):4291-4. doi: 10.1016/j.bmcl.2005.06.050.
Kofi A Oppong 1,  Christopher D Ellis,  Michael C Laufersweiler,  Steven V O'Neil,  Yili Wang,  David L Soper,  Mark W Baize,  John A Wos,  Biswanath De,  Gregory K Bosch,  Amy N Fancher,  Wei Lu,  Maureen K Suchanek,  Richard L Wang,  Thomas P Demuth Jr
Affiliations

Affiliation

  • 1 Procter & Gamble Pharmaceuticals, Inc., 8700 Mason-Montgomery Road, Mason, OH 45040, USA. Oppong.ka@pg.com
PMID: 16046125 DOI: 10.1016/j.bmcl.2005.06.050
Abstract

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-1beta.

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