5,5-二苯基咪唑啉酮作为强效人神经肽Y5受体拮抗剂的合成与评价
Synthesis and evaluation of 5,5-diphenylimidazolones as potent human neuropeptide Y5 receptor antagonists.
作者信息
Gillman Kevin W, Higgins Mendi A, Poindexter Graham S, Browning Marc, Clarke Wendy J, Flowers Sharon, Grace James E, Hogan John B, McGovern Rachel T, Iben Lawrence G, Mattson Gail K, Ortiz Astrid, Rassnick Stefanie, Russell John W, Antal-Zimanyi Ildiko
机构信息
Bristol-Myers Squibb Pharmaceutical Research Institute, Richard L. Gelb Center for Pharmaceutical Research and Development, Wallingford, CT 06492, USA.
出版信息
Bioorg Med Chem. 2006 Aug 15;14(16):5517-26. doi: 10.1016/j.bmc.2006.04.042. Epub 2006 May 11.
A series of novel 5,5-diphenylimidazolones was synthesized and evaluated for activity against the human neuropeptide Y5 receptor. The 3-pyridyl analog 46 demonstrated an IC(50) of 8.3 nM with a favorable pharmacokinetic profile in rats, but was ineffective in reducing food intake.
合成了一系列新型的5,5-二苯基咪唑啉酮，并对其针对人神经肽Y5受体的活性进行了评估。3-吡啶基类似物46在大鼠中显示出8.3 nM的半数抑制浓度（IC50），且具有良好的药代动力学特征，但在减少食物摄入量方面无效。
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