作为GABAA受体α/β界面配体的C2取代咪唑并喹啉的新型合成方法。
Novel synthetic procedures for C2 substituted imidazoquinolines as ligands for the α/β-interface of the GABAA-receptor.
作者信息
Draskovits Markus, Catorci Daniele, Wimmer Laurin, Rehman Sabah, Siebert David Chan Bodin, Ernst Margot, Schnürch Michael, Mihovilovic Marko D
机构信息
Institute of Applied Synthetic Chemistry, TU Wien, Getreidemarkt 9/163, 1060 Vienna, Austria.
Center for Brain Research, Medical University of Vienna, Spitalgasse 4, 1090 Vienna, Austria.
出版信息
Monatsh Chem. 2023;154(12):1391-1404. doi: 10.1007/s00706-022-02988-8. Epub 2022 Oct 29.
UNLABELLED
A series of substituted imidazoquinolines, a structurally related chemotype to pyrazoloquinolinones, a well-known class of GABA ligands, was prepared via two synthetic procedures and the efficiency of these procedures were compared. One method relies on classical heterocyclic synthesis, the other one aims at late-stage decoration of a truncated scaffold via direct C-H functionalization. A pharmacological evaluation disclosed that one of the synthesized derivatives showed interesting activity on a α1β3 containing receptor subtype.
SUPPLEMENTARY INFORMATION
The online version contains supplementary material available at 10.1007/s00706-022-02988-8.
未标记
通过两种合成方法制备了一系列取代咪唑喹啉，其为结构上与吡唑并喹啉酮相关的化学类型，吡唑并喹啉酮是一类著名的GABA配体，并比较了这些方法的效率。一种方法依赖于经典的杂环合成，另一种方法旨在通过直接C-H官能化对截短的支架进行后期修饰。药理学评估表明，其中一种合成衍生物对含α1β3的受体亚型表现出有趣的活性。
补充信息
在线版本包含可在10.1007/s00706-022-02988-8获取的补充材料。
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