Synthesis and biological evaluation of 5-nitropyrimidine analogs with azabicyclic substituents as GPR119 agonists

Z Yang, Y Fang, TAN Pham, J Lee, H Park

文献索引：Yang, Zunhua; Fang, Yuanying; Pham, Tuan-Anh N.; Lee, Jongkook; Park, Haeil Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 5 p. 1519 - 1521

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被引用次数: 7

摘要

5-Nitropyrimidine analogs substituted with conformationally restricted azabicyclic amines and alcohols were prepared and evaluated their agonistic activity against human GPR119. The analogs bearing endo-azabicyclic amines and alcohols (7, 8, 11, and 12) exhibited full agonistic activities while the analogs with exo-azabicyclic amines and alcohols were proved as partial agonists (9, 10, 13, and 14) regardless of their EC50 values. 5-Nitropyrimidine ...