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

…, O Okamoto, H Iwaasa, A Gomori, A Ishihara…

Index: Sato, Nagaaki; Jitsuoka, Makoto; Ishikawa, Shiho; Nagai, Keita; Tsuge, Hiroyasu; Ando, Makoto; Okamoto, Osamu; Iwaasa, Hisashi; Gomori, Akira; Ishihara, Akane; Kanatani, Akio; Fukami, Takehiro Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 6 p. 1670 - 1674

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Citation Number: 10

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 IC50 of 54nM. Subsequent optimization led to the identification of several potent derivatives.