Discovery of substituted 2,4,4-triarylimidazoline derivatives as potent and selective neuropeptide Y Y5 receptor antagonists |
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| Authors: | Nagaaki Sato Makoto Jitsuoka Shiho Ishikawa Keita Nagai Hiroyasu Tsuge Makoto Ando Osamu Okamoto Hisashi Iwaasa Akira Gomori Akane Ishihara Akio Kanatani Takehiro Fukami |
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| Institution: | Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Company, Ltd, 3 Okubo, Tsukuba 300-2611, Japan |
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| 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 54 nM. Subsequent optimization led to the identification of several potent derivatives. |
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