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

Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinylimidazoles 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 provid...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2013-04, Vol.23 (7), p.2134-2139
Hauptverfasser:	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
Format:	Artikel
Sprache:	eng
Schlagworte:	Allosteric Regulation - drug effects amides Amides - chemical synthesis Amides - chemistry Amides - pharmacology Animals Antidepressant Binding Sites - drug effects chemistry Dose-Response Relationship, Drug Drug Discovery HEK293 Cells Humans Imidazole amide imidazoles Imidazoles - chemical synthesis Imidazoles - chemistry Imidazoles - pharmacology Ligand-lipophilic efficiency (LipE) Ligands Metabotropic glutamate receptor 5 (mGluR5) Mice Models, Molecular Molecular Structure Negative allosteric modulators Pyrazole amide Pyrazoles - chemical synthesis Pyrazoles - chemistry Pyrazoles - pharmacology Rats Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate - antagonists & inhibitors Structure-Activity Relationship
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Zusammenfassung:	Development of SAR in a 5-aryl-3-acylpyridinyl-pyrazoles and 1-aryl-4-acylpyridinylimidazoles 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. 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.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2013.01.116