title: Design, syntheses, and structure-activity relationships of novel NPY Y5 receptor antagonists: 2-{3-Oxospiro[isobenzofuran-1(3H),4'-piperidin]-1'-yl}benzimidazole derivatives.
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, orally available, and brain-penetrable Y5 selective antagonist (5k).
authors: Banyu Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo-3, Tsukuba 300-2611, Ibaraki, Japan.
authors: Yoshio
authors: Y
authors: Ogino
authors: Norikazu
authors: N
authors: Ohtake
authors: Yoshikazu
authors: Y
authors: Nagae
authors: Kenji
authors: K
authors: Matsuda
authors: Minoru
authors: M
authors: Moriya
authors: Takuya
authors: T
authors: Suga
authors: Makoto
authors: M
authors: Ishikawa
authors: Maki
authors: M
authors: Kanesaka
authors: Yuko
authors: Y
authors: Mitobe
authors: Junko
authors: J
authors: Ito
authors: Tetsuya
authors: T
authors: Kanno
authors: Akane
authors: A
authors: Ishihara
authors: Hisashi
authors: H
authors: Iwaasa
authors: Tomoyuki
authors: T
authors: Ohe
authors: Akio
authors: A
authors: Kanatani
authors: Takehiro
authors: T
authors: Fukami
mesh_terms: D000284:Administration, Oral; D000818:Animals; D001562:Benzimidazoles / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D001921:Brain / Q000187:drug effects; D020650:Combinatorial Chemistry Techniques; D015195:Drug Design; D015394:Molecular Structure; D051381:Rats; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors*; D013329:Structure-Activity Relationship
chemical_list: D001562:Benzimidazoles; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor