Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators

…, NR Cho, KH Lee, HJ Jeong, SJ Kim, Y Choi…

Index: Chae, Eunhee; Shin, Yong-Je; Ryu, Eun-Ju; Ji, Mi Kyung; Ryune Cho, Nahm; Lee, Ki-Ho; Jeong, Hyun Ji; Kim, Soo-Jin; Choi, Yeonjung; Seok Oh, Kyung; Park, Chun-Eung; Soo Yoon, Young Bioorganic and Medicinal Chemistry Letters, 2013 , vol. 23, # 7 p. 2134 - 2139

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Citation Number: 9

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.