Harper Bart H, Wang Liping, Zhu Cheng, Kar Nam F, Li Bing, Moyes Christopher R, Goble Stephen D, Costa Melissa, Dingley Karen, Di Salvo Jerry, Ha Sookhee N, Hurley Amanda, Li Xiaofang, Miller Randy R, Nagabukuro Hiroshi, Salituro Gino M, Smith Sean, Struthers Mary, Hale Jeffrey J, Edmondson Scott D, Berger Richard
Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
Merck & Co., Inc., 126 E. Lincoln Ave., Rahway, NJ 07065, United States.
Bioorg Med Chem Lett. 2017 Feb 15;27(4):1094-1098. doi: 10.1016/j.bmcl.2016.12.033. Epub 2016 Dec 11.
The synthesis of a novel class of piperazine benzamide (reverse amides) targeting the human β-adrenergic receptor for the treatment of overactive bladder (OAB) is described. The SAR studies directed towards maintaining well established β potency and selectivities while improving the overall pharmacokinetic profile in the reverse amide class will be evaluated. The results and consequences associated with functional activity at the norepinephrine transporter (NET) will also be discussed.
描述了一类新型哌嗪苯甲酰胺（反向酰胺）的合成，该类化合物靶向人β-肾上腺素能受体用于治疗膀胱过度活动症（OAB）。将评估旨在维持已确立的β效能和选择性，同时改善反向酰胺类整体药代动力学特征的构效关系（SAR）研究。还将讨论与去甲肾上腺素转运体（NET）功能活性相关的结果及影响。
