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新型6-芳基异吲哚啉-1-酮衍生物作为代谢型谷氨酸受体2的负变构调节剂

Novel 6-Aryl isoindolin-1-one Derivatives as Negative Allosteric Modulators of Metabotropic Glutamate Receptor 2.

作者信息

Li Yinlong, Liang Steven H

机构信息

Department of Radiology and Imaging Sciences, Emory University, 1364 Clifton Road, Atlanta, Georgia 30322, United States.

出版信息

ACS Med Chem Lett. 2025 Mar 19;16(4):510-511. doi: 10.1021/acsmedchemlett.5c00107. eCollection 2025 Apr 10.

Abstract

This highlight describes a series of novel 6-aryl isoindolin-1-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor 2 (mGluR). The chemical synthesis, selectivity over mGluR, and pharmaceutical compositions of those compounds are disclosed.

摘要

本亮点介绍了一系列新型6-芳基异吲哚啉-1-酮衍生物,作为代谢型谷氨酸受体2(mGluR)的负变构调节剂(NAMs)。公开了这些化合物的化学合成、对mGluR的选择性以及药物组合物。

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本文引用的文献

1
Exploring the activation mechanism of metabotropic glutamate receptor 2.
Proc Natl Acad Sci U S A. 2024 May 21;121(21):e2401079121. doi: 10.1073/pnas.2401079121. Epub 2024 May 13.
2
Sex differences and hormonal regulation of metabotropic glutamate receptor synaptic plasticity.
Int Rev Neurobiol. 2023;168:311-347. doi: 10.1016/bs.irn.2022.10.002. Epub 2022 Nov 11.
3
Challenges in the Discovery and Optimization of mGlu Heterodimer Positive Allosteric Modulators.
Lett Drug Des Discov. 2019 Dec;16(12):1387-1394. doi: 10.2174/1570180815666181017131349.

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