二苯并[b,f][1,5]噁嗪衍生物的合成及对κ-阿片受体激动活性的生物评价。
Synthesis and biological evaluation of dibenz[b,f][1,5]oxazocine derivatives for agonist activity at κ-opioid receptor.
机构信息
Chemistry Division, Indian Institute of Chemical Biology, 4, Raja S.C. Mullick Road, Kolkata 700 032, India.
出版信息
Eur J Med Chem. 2011 May;46(5):1713-20. doi: 10.1016/j.ejmech.2011.02.024. Epub 2011 Feb 22.
PMID:21392859
Abstract
A short and high yield synthetic route to dibenz[b,f][1,5]oxazocines has been developed using Pd catalyzed intramolecular cycloamination reaction. Receptor binding assay using [125I]-dynorphin demonstrated that one of the derivative, 5b showed selective κ-opioidergic property.
摘要
一种短而高产的二苯并[b,f][1,5]噁嗪类化合物的合成路线已经开发出来，该路线采用 Pd 催化的分子内环化胺化反应。使用 [125I]-强啡肽进行受体结合测定表明，其中一种衍生物 5b 表现出选择性 κ-阿片样物质特性。
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