期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 13, 期 6, 页码 1901-1911出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2005.01.022
关键词
acetylcholinesterase inhibitor; pyrrolos[3,2,1-ij]quinolin-4-one; rhythmic bladder contraction; TAK-802
As part of an on-going investigation to develop an increasing agent on rhythmic bladder contractions, 1-aryl-3-(1-benzylpiperidin-4-yl)propanones were synthesized and examined as noncarbamate acetylcholinesterase (AChE) inhibitors. Among compounds with various aryl groups, 1,2,5,6-tetrahydro-4H-pyrrolo [3,2,1-ij]quinolin-4-one derivative 9c was found to possess a potent AChE inhibition activity with an IC50 value of 1.3 nM. The compound 9c increased rhythmic bladder contractions in Guinea pigs and rats without affecting the basal intravesical pressure, which suggests that 9c may be useful for the treatment of voiding dysfunction caused by detrusor underactivity. (c) 2005 Elsevier Ltd. All rights reserved.
作者
我是这篇论文的作者
点击您的名字以认领此论文并将其添加到您的个人资料中。
推荐
暂无数据