Design, syntheses, and structure–activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro [isobenzofuran-1 (3H), 4′-piperidin]-1′-yl} …

…, Y Mitobe, J Ito, T Kanno, A Ishihara, H Iwaasa…

文献索引：Ogino, Yoshio; Ohtake, Norikazu; Nagae, Yoshikazu; Matsuda, Kenji; Moriya, Minoru; Suga, Takuya; Ishikawa, Makoto; Kanesaka, Maki; Mitobe, Yuko; Ito, Junko; Kanno, Tetsuya; Ishihara, Akane; Iwaasa, Hisashi; Ohe, Tomoyuki; Kanatani, Akio; Fukami, Takehiro Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 18 p. 5010 - 5014

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被引用次数: 39

摘要

Design, syntheses, and structure–activity relationships of a novel class of 2-{3-oxospiro [isobenzofuran-1 (3H), 4′-piperidin]-1′-yl} benzimidazole NPY Y5 receptor antagonists are described. The benzimidazole structures were newly designed based on the urea linkage of our prototype Y5 receptor antagonists (2 and 3). By optimizing substituents on the benzimidazole core part of the lead compound 5a, we were able to develop a potent, ...