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Synthesis and biological evaluation of novel 2,4-disubstituted quinazoline analogues as GPR119 agonists

  作者 PHAM TUANANH N; YANG ZUNHUA; FANG YUANYING; LUO JUN; LEE JONGKOOK; PARK HAEIL  
  选自 期刊  Bioorganic & Medicinal Chemistry;  卷期  2013年21-5;  页码  1349-1356  
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[摘要]GPR119 agonist has emerged as a promising target for the treatment of type 2 diabetes. A series of novel 2,4-disubstituted quinazoline analogues was prepared and evaluated their agonistic activity against human GPR119. The analogues bearing azabicyclic amine substituents (12a, 12c and 12g) exhibited better EC50 values than that of OEA though they appeared to be partial agonists. (C) 2012 Elsevier Ltd. All rights reserved.

 
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