C2取代咪唑喹啉作为gabaa受体α/β界面配体的新合成方法。

IF 0.6 4区工程技术 Q4 ENGINEERING, CHEMICAL

Journal of Chemical Engineering of Japan Pub Date : 2023-01-01 Epub Date: 2022-10-29 DOI:10.1007/s00706-022-02988-8

Markus Draskovits, Daniele Catorci, Laurin Wimmer, Sabah Rehman, David Chan Bodin Siebert, Margot Ernst, Michael Schnürch, Marko D Mihovilovic

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引用次数: 0

摘要

通过两种不同的合成方法制备了一系列与GABAA配体吡唑喹啉酮结构相似的取代咪唑喹啉类化合物，并比较了两种合成方法的效率。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碳氢功能化对截断支架进行后期修饰。药理学评价表明，其中一个合成的衍生物对含有α1β3受体亚型具有有趣的活性。图片摘要:补充资料:在线版本包含补充资料，网址为10.1007/s00706-022-02988-8。

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Novel synthetic procedures for C2 substituted imidazoquinolines as ligands for the α/β-interface of the GABAA-receptor.

A series of substituted imidazoquinolines, a structurally related chemotype to pyrazoloquinolinones, a well-known class of GABA_A 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.

Graphical abstract:

Supplementary information: The online version contains supplementary material available at 10.1007/s00706-022-02988-8.

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来源期刊

Journal of Chemical Engineering of Japan 工程技术-工程：化工

CiteScore

1.70

自引率

12.50%

发文量

审稿时长

1.9 months

期刊介绍： The Journal of Chemical Engineering of Japan (JCEJ) is a monthly publication in English of the Society of Chemical Engineers, Japan. The first issue appeared in 1968. JCEJ publishes timely original research in the broad field of chemical engineering ranging from fundamental principles to practical applications. JCEJ is an international research journal and invites your contributions and subscriptions. All areas of chemical engineering are covered, including: Physical Properties and Physical Chemistry, Transport Phenomena and Fluid Engineering, Particle Engineering, Separation Engineering, Thermal Engineering, Chemical Reaction Engineering, Process Systems Engineering and Safety, Biochemical, Food and Medical Engineering, Micro and Nano Systems, Materials Engineering and Interfacial Phenomena, Energy, Environment, and Engineering Education.