title: Novel potent antagonists of human neuropeptide Y-Y5 receptor. Part 4: tetrahydrodiazabenzazulene derivatives.
abstract: Novel tetrahydrodiazabenzazulene derivatives, designed from the lead compound 1 discovered by screening of our in-house chemical library, were prepared and found to be potent neuropeptide Y-Y5 (NPY-Y5) receptor antagonists. The structure-activity relationships are described. Compounds 7 (FR240662) and 16 (FR252384) were especially attractive owing to their high affinities for the NPY-Y5 receptors, oral absorption and permeability to brain.
authors.affiliation: Medicinal Chemistry Research Laboratories, Fujisawa Pharmaceutical Co., Ltd., 2-1-6 Kashima, Yodogawa-ku, Osaka 532-8514, Japan. yoshinaro_sato@po.fujisawa.co.jp
authors.forename: Yoshinari
authors.initials: Y
authors.lastname: Satoh
authors.forename: Chie
authors.initials: C
authors.lastname: Hatori
authors.forename: Harunobu
authors.initials: H
authors.lastname: Ito
mesh_terms: D000284:Administration, Oral; D000818:Animals; D052176:Azulenes; D019817:Benzoic Acid / Q000737:chemistry; D001665:Binding Sites; D001921:Brain / Q000187:drug effects / Q000378:metabolism; D003508:Cycloheptanes / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D004435:Eating; D006571:Heterocyclic Compounds / Q000138:chemical synthesis / Q000494:pharmacology; D008958:Models, Molecular; D010539:Permeability / Q000187:drug effects; D051381:Rats; D011924:Rats, Zucker; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D052176:Azulenes; D003508:Cycloheptanes; D006571:Heterocyclic Compounds; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; C005525:azulene; D019817:Benzoic Acid