Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists

JeonM.-K.; LeeK.M.; KimI.H.; JangY.K.; KangS.K.; LeeJ.M.; JungK.-Y.; KumarJ.A.; RheeS.D.; JungW.H.; SongJ.S.; BaeM.A.; KimK.R.; AhnJ.H.

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Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists

机译：硫代嘧啶衍生物作为GPR119激动剂的合成及生物学评价

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A series of thienopyrimidine derivatives was synthesized and evaluated for their GPR119 agonistic ability. Several thienopyrimidine derivatives containing R1 and R2 substituents displayed potent GPR119 agonistic activity. Among them, compound 5d, which is a prototype, showed good in vitro activity with an EC50 value of 3 nM and human and rat liver microsomal stability. Compound 5d exhibited no CYP inhibition and induction, Herg binding, or mutagenic potential. Compound 5d showed increase insulin secretion in beta TC-6 cell and lowered the glucose excursion in mice in an oral glucose-tolerance test.

机译：合成了一系列噻吩并嘧啶衍生物，并评估了它们的GPR119激动能力。几个含有R1和R2取代基的噻吩并嘧啶衍生物显示出强大的GPR119激动活性。其中，作为原型的化合物5d表现出良好的体外活性，EC50值为3 nM，具有人和大鼠肝脏微粒体的稳定性。化合物5d没有显示CYP抑制和诱导，Herg结合或诱变潜能。在口服葡萄糖耐量试验中，化合物5d显示增加了βTC-6细胞中的胰岛素分泌，并降低了小鼠的葡萄糖偏移。

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《Bioorganic and Medicinal Chemistry Letters》 |2014年第17期|共5页
作者
JeonM.-K.; LeeK.M.; KimI.H.; JangY.K.; KangS.K.; LeeJ.M.; JungK.-Y.; KumarJ.A.; RheeS.D.; JungW.H.; SongJ.S.; BaeM.A.; KimK.R.; AhnJ.H.;
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正文语种 eng
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Diabetes; GPR119; Thienopyrimidine; Treatment;

机译：糖尿病;GPR119;硫嘧啶;治疗;

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1. Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists [J] . JeonM.-K., LeeK.M., KimI.H., Bioorganic and Medicinal Chemistry Letters . 2014,第17期

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Synthesis and biological evaluation of thienopyrimidine derivatives as GPR119 agonists

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