Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives |
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Authors: | 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 |
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Institution: | Banyu Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan. |
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Abstract: | Design, syntheses, and structure-activity relationships of a novel class of 2-{3-oxospiroisobenzofuran-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, orally available, and brain-penetrable Y5 selective antagonist (5k). |
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