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Updated: May 13, 2026
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Methods for the Discovery of Novel Compounds Modulating a Gamma-Aminobutyric Acid Receptor Type A Neurotransmission
Published on: August 16, 2018
Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators
Eunhee Chae1, Yong-Je Shin, Eun-Ju Ryu
1CNS Drug Discovery, Drug Development Center, SK Biopharmaceuticals, Daejeon 305-712, Republic of Korea. Eunhee.chae@sk.com
Bioorganic & Medicinal Chemistry Letters
|February 26, 2013
Abstract:
Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinyl imidazoles series of mGlu5 receptor negative allosteric modulators (mGluR5 NAMs) using a functional cell-based assay is described in this Letter. Analysis of the Ligand-lipophilic efficiency (LipE) of compounds provided new insight for the design of potent mGluR5 negative allosteric modulators with anti-depressant activities.
