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Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives |
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| Authors: | Takahashi Toshiyuki Sakuraba Aya Hirohashi Tomoko Shibata Takunobu Hirose Masaaki Haga Yuji Nonoshita Katsumasa Kanno Tetsuya Ito Junko Iwaasa Hisashi Kanatani Akio Fukami Takehiro Sato Nagaaki |
| Affiliation: | Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba 300-2611, Japan. |
| 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. |
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