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Synthesis and biological evaluation of 1, 2, 4-oxadiazole derivatives as novel GPR119 agonists.

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机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China [2]Division of Nephrology, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, China

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关键词： agonistic activity cAMP GPCR GPR119 SAR study

摘要：

A series of 1, 2, 4-oxadiazole derivatives have been designed and synthesized, and 25 compounds were evaluated their abilities by the assay of cAMP concentration in GPR119-transfected HEK293T cells. All compounds showed acceptable agonistic effects on GPR119. Among these compounds, 4p exhibited the best agonistic effects with the EC50 of 20.6 nm, which was comparable to that of positive control GPR119 agonist GSK1292263. The agonistic activity of these 1,2,4-oxadiazole derivatives led to the establishment of a structure-activity relationship. © 2016 John Wiley & Sons A/S.

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出版当年[2017]版：

大类 | 3 区医学

小类 | 3 区药物化学 4 区生化与分子生物学

最新[2023]版：

大类 | 4 区医学

小类 | 4 区生化与分子生物学 4 区药物化学

第一作者：

第一作者机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China

通讯作者：

通讯机构： [1]State Key Laboratory of Biotherapy and Cancer Center/Collaborative Innovation Center of Biotherapy, West China Hospital, West China Medical School of Sichuan University, Chengdu, China [2]Division of Nephrology, Kidney Research Institute, West China Hospital of Sichuan University, Chengdu, China [*1]State Key Laboratory of Biotherapy and Kidney Research Institute, West China Hospital, West China Medical School of Sichuan University, Chengdu, China.

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