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Discovery of novel conformationally restricted diazocan peptidomimetics as inhibitors of interleukin-1beta synthesis |
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| Authors: | Oppong Kofi A Ellis Christopher D Laufersweiler Michael C O'Neil Steven V Wang Yili Soper David L Baize Mark W Wos John A De Biswanath Bosch Gregory K Fancher Amy N Lu Wei Suchanek Maureen K Wang Richard L Demuth Thomas P |
| Institution: | Procter & Gamble Pharmaceuticals, Inc., 8700 Mason-Montgomery Road, Mason, OH 45040, USA. Oppong.ka@pg.com |
| 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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