16919461 |
Takahashi T, Sakuraba A, Hirohashi T, Shibata T, Hirose M, Haga Y, Nonoshita K, Kanno T, Ito J, Iwaasa H, Kanatani A, Fukami T, Sato N: Novel potent neuropeptide Y Y5 receptor antagonists: synthesis and structure-activity relationships of phenylpiperazine derivatives. Bioorg Med Chem. 2006 Nov 15;14(22):7501-11. 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. |
83(1,1,1,3) |