Discovery of a highly potent series of oxazole-based phosphodiesterase 4 inhibitors
- 作者：Rongze Kuang ; Ho-Jane Shue ; David J. Blythin ; Neng-Yang Shih ; Danlin Gu ; Xiao Chen ; John Schwerdt ; Ling Lin ; Pauline C. Ting ; Xiaohong Zhu ; Robert Aslanian ; John J. Piwinski ; Li Xiao ; Daniel Prelusky
- 关键词：Phosphodiesterase 4 ; PDE4 inhibitor ; Oxazole ; Quinoline ; Anti-inflammatory ; COPD
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2007
- 期刊代码：10_0960894x
- 类别：ch
- 出版时间：15 September 2007
- 卷：17
- 期：18
- 页码：5150-5154
- 文件大小：236 K
摘要
Substituted quinolyl oxazoles were discovered as a novel and highly potent series of phosphodiesterase 4 (PDE4) inhibitors. Structure–activity relationship studies revealed that the oxazole core, with 4-carboxamide and 5-aminomethyl groups, is a novel PDE4 inhibitory pharmacophore. Selectivity profiles and in vivo biological activity are also reported.