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ID: ALA2311488

Journal: Bioorg Med Chem Lett

Title: Identification of a novel benzimidazole derivative as a highly potent NPY Y5 receptor antagonist with an anti-obesity profile.

Authors: Tamura Y, Hayashi K, Omori N, Nishiura Y, Watanabe K, Tanaka N, Fujioka M, Kouyama N, Yukimasa A, Tanaka Y, Chiba T, Tanioka H, Nambu H, Yukioka H, Sato H, Okuno T.

Abstract: Optimization of HTS hit 1 for NPY Y5 receptor binding affinity, CYP450 inhibition, solubility and metabolic stability led to the identification of some orally available oxygen-linker derivatives for in vivo study. Among them, derivative 4i inhibited food intake induced by the NPY Y5 selective agonist, and chronic oral administration of 4i in DIO mice caused a dose-dependent reduction of body weight gain.

CiteXplore: 23206862

DOI: 10.1016/j.bmcl.2012.11.005