Sato Nagaaki, Jitsuoka Makoto, Ishikawa Shiho, Nagai Keita, Tsuge Hiroyasu, Ando Makoto, Okamoto Osamu, Iwaasa Hisashi, Gomori Akira, Ishihara Akane, Kanatani Akio, Fukami Takehiro
Tsukuba Research Institute, Merck Research Laboratories, Banyu Pharmaceutical Company, Ltd, 3 Okubo, Tsukuba 300-2611, Japan.
Bioorg Med Chem Lett. 2009 Mar 15;19(6):1670-4. doi: 10.1016/j.bmcl.2009.01.101. Epub 2009 Feb 4.
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.
新型咪唑啉衍生物被发现是有效的神经肽Y Y5受体拮抗剂。针对人类Y5受体对默克样品库进行高通量筛选，结果鉴定出2,4,4-三苯基咪唑啉（1），其IC50为54 nM。随后的优化导致鉴定出几种有效的衍生物。
