Literature DB >> 23434029

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

Eunhee Chae1, 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.   

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.
Copyright © 2013 Elsevier Ltd. All rights reserved.

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Year:  2013        PMID: 23434029     DOI: 10.1016/j.bmcl.2013.01.116

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

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Authors:  Agostinho Lemos; Rita Melo; Antonio Jose Preto; Jose Guilherme Almeida; Irina Sousa Moreira; Maria Natalia Dias Soeiro Cordeiro
Journal:  Curr Neuropharmacol       Date:  2018       Impact factor: 7.363

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Authors:  Elizabeth O'Bryan McCusker; Karl A Scheidt
Journal:  Angew Chem Int Ed Engl       Date:  2013-11-18       Impact factor: 15.336

4.  Fragment-Based Lead Generation of 5-Phenyl-1H-pyrazole-3-carboxamide Derivatives as Leads for Potent Factor Xia Inhibitors.

Authors:  Qunchao Wei; Zhichao Zheng; Shijun Zhang; Xuemin Zheng; Fancui Meng; Jing Yuan; Yongnan Xu; Changjiang Huang
Journal:  Molecules       Date:  2018-08-10       Impact factor: 4.411

  4 in total

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