Synthesis and structure–activity relationship of 4-amino-2-phenylpyrimidine derivatives as a series of novel GPR119 agonists

K Negoro, Y Yonetoku, T Maruyama, S Yoshida…

Index: Negoro, Kenji; Yonetoku, Yasuhiro; Maruyama, Tatsuya; Yoshida, Shigeru; Takeuchi, Makoto; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 7 p. 2369 - 2375

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Citation Number: 13

Abstract

Through preparation and examination of a series of novel 4-amino-2-phenylpyrimidine derivatives as agonists for GPR119, we identified 2-(4-bromophenyl)-6-methyl-N-[2-(1- oxidopyridin-3-yl) ethyl] pyrimidin-4-amine (9t). Compound 9t improved glucose tolerance in mice following oral administration and showed good pharmacokinetic profiles in rats.