Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents
详细信息 查看全文
- 作者：Gang Li1 ; Yi Huan1 ; Baokun Yuan ; Jin Wang ; Qian Jiang ; Ziyun Lin ; Zhufang Shen ; shenzhf@imm.ac.cn" class="auth_mail" title="E-mail the corresponding author ; Haihong Huang ; joyce@imm.ac.cn" class="auth_mail" title="E-mail the corresponding author
- 关键词：Xanthine derivatives ; Dual ligands ; DPP-IV ; GPR119 ; Merged pharmacophores
- 刊名：European Journal of Medicinal Chemistry
- 出版年：2016
- 出版时间：29 November 2016
- 年：2016
- 卷：124
- 期：Complete
- 页码：103-116
- 全文大小：2341 K
文摘
- •
A series of xanthine derivatives targeting DPP-IV and GPR119 was synthesized.
- •
Systematic optimization led to the identification of dual modulator 20i.
- •
Compound 20i had a selective DPP-IV inhibition and good GPR119 agonism activity.
- •
Compound 20i had a favorable metabolic stability.
- •
Insulinotropic effect of compound 20i was glucose-concentration dependent.