Dual function inhibitors of relevance to chronic obstructive pulmonary disease

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS

卷:21

Article

Dou, Dengfeng¹  He, Guijia¹  Alliston, Kevin R.¹  Groutas, William C.¹ 

[1] Wichita State Univ, Dept Chem, Wichita, KS 67260 USA

关键词: Elastase;    Caspase-1;    ICE;    Inhibitor;    Dual function;   

DOI  :  10.1016/j.bmcl.2010.12.033

来源: Elsevier

【 摘 要 】

The general strategy and rationale underlying the design of COPD therapeutics that possess protease inhibitory activity and are also capable of releasing a species that attenuates inflammation by inhibiting caspase-1, are described. The synthesis and in vitro biochemical evaluation of a dual function molecule that sequentially inhibits HNE and caspase-1 in a time-dependent manner is reported. (C) 2010 Elsevier Ltd. All rights reserved.

【 授权许可】

Free