Literature DB >> 16837196

Structure-activity relationships for the linker in a series of pyridinyl-alkynes that are antagonists of the metabotropic glutamate receptor 5 (mGluR5).

Peter Bach1, Karolina Nilsson, Tor Svensson, Udo Bauer, Lance G Hammerland, Alecia Peterson, Andreas Wållberg, Krister Osterlund, David Karis, Maria Boije, David Wensbo.   

Abstract

Studies of structure-activity relationships for the linker in a new series of metabotropic glutamate receptor 5 antagonists are presented together with in vitro and in vivo pharmacokinetic data.

Entities:  

Mesh：

Substances：

Year:  2006        PMID： 16837196     DOI： 10.1016/j.bmcl.2006.06.078

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


  4 in total

1.  Structure-activity relationships comparing N-(6-methylpyridin-yl)-substituted aryl amides to 2-methyl-6-(substituted-arylethynyl)pyridines or 2-methyl-4-(substituted-arylethynyl)thiazoles as novel metabotropic glutamate receptor subtype 5 antagonists.

Authors:  Santosh S Kulkarni; Mu-Fa Zou; Jianjing Cao; Jeffrey R Deschamps; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal:  J Med Chem       Date:  2009-06-11       Impact factor: 7.446

2.  Synthesis and SAR of novel, non-MPEP chemotype mGluR5 NAMs identified by functional HTS.

Authors:  Ya Zhou; Alice L Rodriguez; Richard Williams; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-10-28       Impact factor: 2.823

3.  Structure-activity relationships in a novel series of 7-substituted-aryl quinolines and 5-substituted-aryl benzothiazoles at the metabotropic glutamate receptor subtype 5.

Authors:  Peng Zhang; Mu-Fa Zou; Alice L Rodriguez; P Jeffrey Conn; Amy Hauck Newman
Journal:  Bioorg Med Chem       Date:  2010-03-27       Impact factor: 3.641

4.  Discovery and SAR of novel mGluR5 non-competitive antagonists not based on an MPEP chemotype.

Authors:  Alice L Rodriguez; Richard Williams; Ya Zhou; Stacey R Lindsley; Uyen Le; Mark D Grier; C David Weaver; P Jeffrey Conn; Craig W Lindsley
Journal:  Bioorg Med Chem Lett       Date:  2009-05-03       Impact factor: 2.823
  4 in total

北京卡尤迪生物科技股份有限公司 © 2022-2023.