Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators |
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| Authors: | Eunhee Chae Yong-Je Shin Eun-Ju Ryu Mi Kyung Ji Nahm Ryune Cho Ki-Ho Lee Hyun Ji Jeong Soo-Jin Kim Yeonjung Choi Kyung Seok Oh Chun-Eung Park Young Soo Yoon |
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| Institution: | CNS Drug Discovery, Drug Development Center, SK Biopharmaceuticals, Daejeon 305-712, Republic of Korea |
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| 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. |
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