Author/Authors :
Toshihiro Sakamoto، نويسنده , , Minoru Moriya، نويسنده , , Hiroyasu Tsuge، نويسنده , , Toshiyuki Takahashi، نويسنده , , Yuji Haga، نويسنده , , Katsumasa Nonoshita، نويسنده , , Osamu Okamoto، نويسنده , , Hirobumi Takahashi، نويسنده , , Aya Sakuraba، نويسنده , , Tomoko Hirohashi، نويسنده , , Takunobu Shibata، نويسنده , , Tetsuya Kanno، نويسنده , , Junko Ito، نويسنده , , Hisashi Iwaasa، نويسنده , , Akira Gomori، نويسنده , , Akane Ishi، نويسنده ,
Abstract :
Spiroindoline urea derivatives, designed to act as NPY Y5 receptor antagonists, were synthesized and their structure–activity relationships were investigated. Of these derivatives, compound 3a showed good Y5 binding affinity with favorable pharmacokinetic properties. Compound 3a significantly inhibited bPP Y5 agonist-induced food intake in rats, and suppressed body weight gain in DIO mice.
Keywords :
Neuropeptide Y , NPY , Y5 receptor , Spiroindoline , Obesity , Phenyl imidazole
