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
Tsukuba Research Institute, Banyu Pharmaceutical Co., Ltd, Okubo 3, Tsukuba 300-2611, Japan.
Bioorg Med Chem. 2006 Nov 15;14(22):7501-11. doi: 10.1016/j.bmc.2006.07.023. Epub 2006 Aug 17.
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.
合成了一系列苯哌嗪衍生物，并对其神经肽Y（NPY）Y5受体拮抗活性进行了评估。将2的苯茚部分替换为1-苯基哌嗪，得到新型脲衍生物3f。随后通过苯基部分的取代对苯哌嗪模板进行优化，得到了一系列对Y5受体显示出强效结合亲和力和拮抗活性的（2-甲磺酰胺基苯基）哌嗪衍生物。
