Diphenylpyridylethanamine (DPPE)-based aminoheterocycles as cholesteryl ester transfer protein inhibitors

详细信息    查看全文

• 作者：Yufeng Wang ; Wu Yang ; Heather J. Finlay ; Lalgudi S. Harikrishnan ; Ji Jiang ; Muthoni G. Kamau ; Katy Van Kirk ; David S. Nirschl ; David S. Taylor ; Alice Ye A. Chen ; Xiaohong Yin ; Paul G. Sleph ; Richard Z. Yang ; Christine S. Huang ; Leonard P. Adam ; R. Michael Lawrence ; Ruth R. Wexler ; Mark E. Salvati
• 关键词：CETP
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：1 February, 2014
• 年：2014
• 卷：24
• 期：3
• 页码：860-864
• 全文大小：1304 K

文摘

A series of diphenylpyridylethanamine-based inhibitors of cholesteryl ester transfer protein with aminoheterocycles appended onto the N-terminus of the chemotype were explored as urea mimetics. Potent compounds were discovered and were further optimized to improve metabolic stability and PXR transactivation profile.