Discovery of oxazole-based PDE4 inhibitors with picomolar potency

详细信息	查看全文 | 推荐本文 |

• 作者：Rongze Kuang^a ; ^{rongze.kuang@merck.com} ; Ho-Jane Shue^a ; Li Xiao^b ; David J. Blythin^a ; Neng-Yang Shih^a ; Xiao Chen^a ; Danlin Gu^a ; John Schwerdt^a ; Ling Lin^a ; Pauline C. Ting^a ; Jianhua Cao^a ; Robert Aslanian^a ; John J. Piwinski^a ; Daniel Prelusky^c ; Ping Wu^d ; Ji Zhang^d ; Xiang Zhang^d ; Chander S. Celly^d ; Motasim Billah^d ; Peng Wang^d
• 关键词：PDE4 inhibitor ; Phosphodiesterase 4 ; Oxazole ; Picomolar ; Inflammation
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2012
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：1 April, 2012
• 卷：22
• 期：7
• 页码：2594-2597
• 文件大小：1172 K

摘要

Optimization of oxazole-based PDE4 inhibitors has led to the discovery of a series of quinolyl oxazoles, with 4-benzylcarboxamide and 5-伪-aminoethyl groups which exhibit picomolar potency against PDE4. Selectivity profiles and in vivo biological activity are also reported.