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

被引：19

作者：

Oppong, KA ^{[1
]}

Ellis, CD ^{[1
]}

Laufersweiler, MC ^{[1
]}

O'Neil, SV ^{[1
]}

Wang, YL ^{[1
]}

Soper, DL ^{[1
]}

Baize, MW ^{[1
]}

Wos, JA ^{[1
]}

De, B ^{[1
]}

Bosch, GK ^{[1
]}

Fancher, AN ^{[1
]}

Lu, W ^{[1
]}

Suchanek, MK ^{[1
]}

Wang, RL ^{[1
]}

Demuth, TP ^{[1
]}

机构：

[1] Procter & Gamble Pharmaceut Inc, Mason, OH 45040 USA

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2005年 / 15卷 / 19期

关键词：

ICE; caspase-1; diazocan; peptidomimetic; interleukin-1; beta;

D O I：

10.1016/j.bmcl.2005.06.050

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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-1 beta. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：4291 / 4294

页数：4

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2-#