新型嘧啶并[2,3-d]嘧啶衍生物的合成与评价及其作为 GPR119 激动剂的活性。
Synthesis and evaluation of novel fused pyrimidine derivatives as GPR119 agonists.
机构信息
National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China.
College of Pharmacy, Jiangxi University of Traditional Chinese Medicine, Nanchang 330004, China.
出版信息
Bioorg Chem. 2019 May;86:103-111. doi: 10.1016/j.bioorg.2019.01.032. Epub 2019 Jan 22.
A novel series of fused pyrimidine derivatives were designed, synthesized and evaluated as GPR119 agonists. Among them, cyclohexene fused compounds (tetrahydroquinazolines) showed greater GPR119 agonistic activities than did dihydrocyclopentapyrimidine and tetrahydropyridopyrimidine scaffolds. Analogues (16, 19, 26, 28, 42) bearing endo-N-Boc-nortropane amine and fluoro-substituted aniline exhibited better EC values (0.27-1.2 μM) though they appeared to be partial agonists.
设计、合成并评价了一系列新型的嘧啶稠合衍生物作为 GPR119 激动剂。其中，环己烯稠合化合物（四氢喹唑啉）比二氢环戊嘧啶和四氢吡啶嘧啶骨架具有更强的 GPR119 激动活性。含有内-N-Boc-降诺文胺和氟取代苯胺的类似物（16、19、26、28、42）表现出更好的 EC 值（0.27-1.2 μM），尽管它们似乎是部分激动剂。
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