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Discovery of biological evaluation of pyrazole/imidazole amides as mGlu5 receptor negative allosteric modulators.
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.
Afiliação
  • Chae E; CNS Drug Discovery, Drug Development Center, SK Biopharmaceuticals, Daejeon 305-712, Republic of Korea. Eunhee.chae@sk.com
Bioorg Med Chem Lett ; 23(7): 2134-9, 2013 Apr 01.
Article em En | MEDLINE | ID: mdl-23434029
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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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Receptores de Glutamato Metabotrópico / Descoberta de Drogas / Amidas / Imidazóis Limite: Animals / Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article
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Texto completo: 1 Coleções: 01-internacional Base de dados: MEDLINE Assunto principal: Pirazóis / Receptores de Glutamato Metabotrópico / Descoberta de Drogas / Amidas / Imidazóis Limite: Animals / Humans Idioma: En Ano de publicação: 2013 Tipo de documento: Article