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…

Index: 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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Citation Number: 39

Abstract

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, ...