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ID: ALA2157871

Journal: Bioorg Med Chem Lett

Title: Identification of a novel and orally available benzimidazole derivative as an NPY Y5 receptor antagonist with in vivo efficacy.

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 lead compound 2 is described, mainly focusing on modification at the C-2 position of the benzimidazole core. Replacement of the phenyl linker of 2 with saturated rings resulted in identification of compound 8b which combines high Y5 receptor binding affinity with a good ADME profile leading to in vivo efficacy.

CiteXplore: 23025998

DOI: 10.1016/j.bmcl.2012.09.025