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Synthesis and evaluation of novel fused pyrimidine derivatives as GPR119 agonists. 2019
Yuanying Fang, and
Lijuan Xiong, and
Jianguo Hu, and
Shaokun Zhang, and
Saisai Xie, and
Liangxing Tu, and
Yang Wan, and
Yi Jin, and
Xiang Li, and
Shaojie Hu, and
Zunhua Yang
National Engineering Research Center for Manufacturing Technology of TCM Solid Preparation, Jiangxi University of Traditional Chinese Medicine, Nanchang 330006, China.
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 EC50 values (0.27-1.2 μM) though they appeared to be partial agonists.
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