Discovery and biological evaluation of novel 4-amino-2-phenylpyrimidine derivatives as potent and orally active GPR119 agonists

…, H Misawa-Mukai, W Hamaguchi, T Maruyama…

Index: Negoro, Kenji; Yonetoku, Yasuhiro; Misawa-Mukai, Hana; Hamaguchi, Wataru; Maruyama, Tatsuya; Yoshida, Shigeru; Takeuchi, Makoto; Ohta, Mitsuaki Bioorganic and Medicinal Chemistry, 2012 , vol. 20, # 17 p. 5235 - 5246

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Citation Number: 9

Abstract

Novel 4-amino-2-phenylpyrimidine derivatives were synthesized and evaluated as GPR119 agonists. Optimization of the substituents on the phenyl ring at the 2-position and the amino group at the 4-position led to the identification of 3, 4-dihalogenated and 2, 4, 5- trihalogenated phenyl derivatives showing potent GPR119 agonistic activity. The advanced analog (2R)-3-{[2-(4-chloro-2, 5-difluorophenyl)-6-ethylpyrimidin-4-yl] amino} propane-1, ...