Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents

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Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents

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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.

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