Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives.
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.
Takahashi
Toshiyuki
T
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba 300-2611, Japan.
Sakuraba
Aya
A
Hirohashi
Tomoko
T
Shibata
Takunobu
T
Hirose
Masaaki
M
Haga
Yuji
Y
Nonoshita
Katsumasa
K
Kanno
Tetsuya
T
Ito
Junko
J
Iwaasa
Hisashi
H
Kanatani
Akio
A
Fukami
Takehiro
T
Sato
Nagaaki
N
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
D010879:Piperazines; D017476:Receptors, Neuropeptide Y; C100568:neuropeptide Y5 receptor; C031503:phenylpiperazine