Design and synthesis of potent and subtype-selective PPARα agonists

详细信息	查看全文 | 推荐本文 |

• 作者：Ranjit C. Desai ; Edward Metzger ; Conrad Santini ; Peter T. Meinke ; James V. Heck ; Joel P. Berger ; Karen L. MacNaul ; Tian-quan Cai ; Samuel D. Wright ; Arun Agrawal et al.
• 刊名：Bioorganic and Medicinal Chemistry Letters
• 出版年：2006
• 期刊代码：10_0960894x
• 类别：ch
• 出版时间：15 March 2006
• 卷：16
• 期：6
• 页码：1673-1678
• 文件大小：158 K

摘要

Beginning with a moderately potent PPARγ agonist 9, a series of potent and highly subtype-selective PPARα agonists was identified through a systematic SAR study. Based on the results of the efficacy studies in the hamster and dog models of dyslipidemia and the desired pharmacokinetic data, the optimized compound 39 was selected for further profiling.