A novel series of potent and selective EP4 receptor ligands: Facile modulation of agonism and antagonism
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- 作者：Michael J. Boyd ; Carl Berthelette ; Jean-Franç ; ois Chiasson ; Patsy Clark ; John Colucci ; Danielle Denis ; Yongxin Han ; Jean-Francois Lé ; vesque ; Marie-Claude Mathieu ; Rino Stocco ; Alex Therien ; St
- 关键词：Prostaglandin E2 ; EP4 ; Inflammation
- 刊名：Bioorganic and Medicinal Chemistry Letters
- 出版年：2011
- 出版时间：1 January 2011
- 年：2011
- 卷：21
- 期：1
- 页码：484-487
- 全文大小：264 K
文摘
A novel series of EP4 ligands, based on a benzyl indoline scaffold, has been discovered. It was found that agonism and antagonism in this series can be easily modulated by minor modifications on the benzyl group. The pharmacokinetic, metabolic and pharmacological profiles of these compounds was explored. It was found that these compounds show good pharmacokinetics in rat and are efficacious in pre-clinical models of pain and inflammation.