Literature DB >> 17936624

Synthesis and SAR comparison of regioisomeric aryl naphthyridines as potent mGlu5 receptor antagonists.

Paul Galatsis1, Koji Yamagata, John A Wendt, Cleo J Connolly, John W Mickelson, Jared B J Milbank, Susan E Bove, Christopher S Knauer, Rachel M Brooker, Corinne E Augelli-Szafran, Roy D Schwarz, Jack J Kinsora, Kenneth S Kilgore.   

Abstract

We describe three novel regioisomeric series of aryl naphthyridine analogs, which are potent antagonists of the Class III GPCR mGlu5 receptor. The synthesis and in vitro and in vivo pharmacological activities of these analogs are discussed.

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Year:  2007        PMID： 17936624     DOI： 10.1016/j.bmcl.2007.09.083

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


  5 in total

1.  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

2.  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

3.  (3-Cyano-5-fluorophenyl)biaryl negative allosteric modulators of mGlu(5): Discovery of a new tool compound with activity in the OSS mouse model of addiction.

Authors:  Craig W Lindsley; Brittney S Bates; Usha N Menon; Satyawan B Jadhav; Alexander S Kane; Carrie K Jones; Alice L Rodriguez; P Jeffrey Conn; Christopher M Olsen; Danny G Winder; Kyle A Emmitte
Journal:  ACS Chem Neurosci       Date:  2011-08-17       Impact factor: 4.418

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

Review 5.  Synthetic Strategies, Reactivity and Applications of 1,5-Naphthyridines.

Authors:  Maria Fuertes; Carme Masdeu; Endika Martin-Encinas; Asier Selas; Gloria Rubiales; Francisco Palacios; Concepcion Alonso
Journal:  Molecules       Date:  2020-07-16       Impact factor: 4.411
  5 in total

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