title: Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives.
abstract: A series of phenylpiperazine derivatives were synthesized and evaluated for their neuropeptide Y (NPY) Y5 receptor antagonistic activities. The benzindane portion of 2 was replaced by 1-phenylpiperazine, resulting in novel urea derivative 3f. Subsequent optimization of the phenylpiperazine template by substitution of the phenyl moiety resulted in a series of (2-methanesulfonamidephenyl)piperazine derivatives that showed potent binding affinity and antagonistic activity for the Y5 receptor.
authors.affiliation: Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba 300-2611, Japan.
authors.forename: Toshiyuki
authors.initials: T
authors.lastname: Takahashi
authors.forename: Aya
authors.initials: A
authors.lastname: Sakuraba
authors.forename: Tomoko
authors.initials: T
authors.lastname: Hirohashi
authors.forename: Takunobu
authors.initials: T
authors.lastname: Shibata
authors.forename: Masaaki
authors.initials: M
authors.lastname: Hirose
authors.forename: Yuji
authors.initials: Y
authors.lastname: Haga
authors.forename: Katsumasa
authors.initials: K
authors.lastname: Nonoshita
authors.forename: Tetsuya
authors.initials: T
authors.lastname: Kanno
authors.forename: Junko
authors.initials: J
authors.lastname: Ito
authors.forename: Hisashi
authors.initials: H
authors.lastname: Iwaasa
authors.forename: Akio
authors.initials: A
authors.lastname: Kanatani
authors.forename: Takehiro
authors.initials: T
authors.lastname: Fukami
authors.forename: Nagaaki
authors.initials: N
authors.lastname: Sato
mesh_terms: D006801:Humans; D015394:Molecular Structure; D010879:Piperazines / Q000138:chemical synthesis / Q000737:chemistry*; D017476:Receptors, Neuropeptide Y / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D010879:Piperazines; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; C031503:phenylpiperazine