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. 2019 May:86:103-111.
doi: 10.1016/j.bioorg.2019.01.032. Epub 2019 Jan 22.

Synthesis and evaluation of novel fused pyrimidine derivatives as GPR119 agonists

Yuanying Fang  1 , Lijuan Xiong  2 , Jianguo Hu  2 , Shaokun Zhang  1 , Saisai Xie  1 , Liangxing Tu  1 , Yang Wan  1 , Yi Jin  3 , Xiang Li  1 , Shaojie Hu  2 , Zunhua Yang  4
Affiliations

Synthesis and evaluation of novel fused pyrimidine derivatives as GPR119 agonists

Yuanying Fang et al. Bioorg Chem. 2019 May.

Abstract

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.

Keywords: Dihydrocyclopentapyrimidine; GPR119 agonists; Tetrahydroquinazoline; endo-N-boc-nortropane amine.

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