Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.

ID: ALA1153312

Journal: Bioorg Med Chem Lett

Title: Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists.

Authors: Sato N, Jitsuoka M, Ishikawa S, Nagai K, Tsuge H, Ando M, Okamoto O, Iwaasa H, Gomori A, Ishihara A, Kanatani A, Fukami T.

Abstract: Novel imidazoline derivatives were discovered to be potent neuropeptide Y Y5 receptor antagonists. High-throughput screening of Merck sample collections against the human Y5 receptor resulted in the identification of 2,4,4-triphenylimidazoline (1), which had an IC(50) of 54nM. Subsequent optimization led to the identification of several potent derivatives.

CiteXplore: 19233647

DOI: 10.1016/j.bmcl.2009.01.101

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