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

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Oppong KA, Ellis CD, Laufersweiler MC, O'Neil SV, Wang Y, Soper DL, Baize MW, Wos JA, De B, Bosch GK, Fancher AN, Lu W, Suchanek MK, Wang RL, Demuth TP Jr

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

Bioorg Med Chem Lett. 2005 Oct 1;15(19):4291-4.

PubMed ID

16046125 [ View in PubMed

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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.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Pralnacasan	Caspase-1	IC 50 (nM)	2	N/A	N/A	Details