GT-949(GT-949) - 药物靶点：EAAT2_在研适应症：中枢神经系统疾病_专利_临床

概要

基本信息

药物类型

小分子化药

别名

靶点

EAAT2

作用机制

EAAT2调节剂(solute carrier family 1 member 2 modulators)

治疗领域

神经系统疾病

在研适应症

中枢神经系统疾病

非在研适应症-

原研机构

The Wistar Institute

在研机构

Drexel University College of Medicine

非在研机构-

最高研发阶段药物发现

首次获批日期-

最高研发阶段(中国)-

特殊审评-

结构

分子式C30H37N7O2

InChIKeyZVWPOIUAPXDLMB-UHFFFAOYSA-N

CAS号460330-27-2

关联

100 项与 GT-949 相关的临床结果

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100 项与 GT-949 相关的转化医学

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100 项与 GT-949 相关的专利（医药）

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1

项与 GT-949 相关的文献（医药）

2024-04-25·Journal of Medicinal Chemistry

Synthesis and Structure–Activity Relationships for Glutamate Transporter Allosteric Modulators

Article

作者: Rawls, Scott M ; Cheng, Mary Hongying ; Fontana, Andréia C K ; Poli, Adi N R ; Bahar, Ivet ; Salvino, Joseph M ; Reeb, Katelyn L ; Srikanth, Yellamelli V V ; Gour, Jitendra ; Ashok, Devipriya ; Khatiwada, Apeksha ; Anastasi, Nicholas

Excitatory amino acid transporters (EAATs) are essential CNS proteins that regulate glutamate levels. Excess glutamate release and alteration in EAAT expression are associated with several CNS disorders. Previously, we identified positive allosteric modulators (PAM) of EAAT2, the main CNS transporter, and have demonstrated their neuroprotective properties in vitro. Herein, we report on the structure-activity relationships (SAR) for the analogs identified from virtual screening and from our medicinal chemistry campaign. This work identified several selective EAAT2 positive allosteric modulators (PAMs) such as compounds 4 (DA-023) and 40 (NA-014) from a library of analogs inspired by GT949, an early generation compound. This series also provides nonselective EAAT PAMs, EAAT inhibitors, and inactive compounds that may be useful for elucidating the mechanism of EAAT allosteric modulation.

100 项与 GT-949 相关的药物交易

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