4-（二甲基氨基）-2-苯基-2-（2-吡啶基）戊酰胺四种立体异构体的合成及其抗胆碱能活性
Synthesis and anticholinergic activity of the four stereoisomers of 4-(dimethylamino)-2-phenyl-2-(2-pyridyl)pentanamide.
作者信息
Oyasu H, Nagano M, Akahane A, Tomoi M, Tada T, Matsuo M
机构信息
R & D Division, Fujisawa Pharmaceutical Company Ltd., Osaka, Japan.
出版信息
J Med Chem. 1994 Apr 29;37(9):1378-81. doi: 10.1021/jm00035a019.
The four stereoisomers of 4-(dimethylamino)-2-phenyl-(2-pyridyl)pentanamide were synthesized, and the absolute configurations were determined by X-ray crystallography. Pharmacological testing for anticholinergic activity revealed great differences in potency among 10 (2R,4R,IC50 = 0.40 microM), 11 (2S,4S,31 microM), 12 (2R,4S,170 microM), and 13 (2S,4R,0.13 microM). A new drug application for the racemate 8 (FK176, vamicamide) has been filed in Japan for the treatment of overactive detrusor syndrome.
合成了4-(二甲基氨基)-2-苯基-(2-吡啶基)戊酰胺的四种立体异构体，并通过X射线晶体学确定了其绝对构型。抗胆碱能活性的药理学测试显示，10（2R,4R，IC50 = 0.40微摩尔）、11（2S,4S，31微摩尔）、12（2R,4S，170微摩尔）和13（2S,4R，0.13微摩尔）之间的效价存在很大差异。外消旋体8（FK176，瓦米卡胺）已在日本提交新药申请，用于治疗逼尿肌过度活动综合征。
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