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ID: ALA2069245
Journal: Bioorg Med Chem Lett
Title: Design, synthesis and identification of novel benzimidazole derivatives as highly potent NPY Y5 receptor antagonists with attractive in vitro ADME profiles.
Authors: Tamura Y, Omori N, Kouyama N, Nishiura Y, Hayashi K, Watanabe K, Tanaka Y, Chiba T, Yukioka H, Sato H, Okuno T.
Abstract: Optimization of our HTS hit 1, mainly focused on modification at the C-2 position of the benzimidazole core, is described. Elimination of the flexible and metabolically labile -S-CH(2)- part and utilization of less lipophilic pyridone substructure led to identification of novel NPY Y5 receptor antagonists 6, which have low to sub-nanomolar Y5 receptor binding affinity with improved CYP450 inhibition profiles, good solubilities and high metabolic stabilities.
CiteXplore: 22853998