Document Report Card

ID: ALA1145971

Journal: J Med Chem

Title: Design and synthesis of the potent, orally available, brain-penetrable arylpyrazole class of neuropeptide Y5 receptor antagonists.

Authors: Sato N, Takahashi T, Shibata T, Haga Y, Sakuraba A, Hirose M, Sato M, Nonoshita K, Koike Y, Kitazawa H, Fujino N, Ishii Y, Ishihara A, Kanatani A, Fukami T.

Abstract: Novel arylpyrazole derivatives were synthesized and evaluated as neuropeptide Y (NPY) Y5 receptor antagonists. Compound (-)-7, which features a novel chiral 2,3-dihydro-1H-cyclopenta[a]naphthalene moiety, showed good binding affinity and antagonistic activity for the Y5 receptor. After intracerebroventricular administration in SD rats, (-)-7 significantly inhibited food intake that was induced by the centrally administered Y5-preferring agonist, bovine pancreatic polypeptide, but had only a negligible effect on NPY-induced feeding.

CiteXplore: 12593644

DOI: 10.1021/jm025513q