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Synthesis and SAR development of novel mGluR1 antagonists for the treatment of chronic pain.
Brumfield, Stephanie; Korakas, Peter; Silverman, Lisa S; Tulshian, Deen; Matasi, Julius J; Qiang, Li; Bennett, Chad E; Burnett, Duane A; Greenlee, William J; Knutson, Chad E; Wu, Wen-Lian; Sasikumar, T K; Domalski, Martin; Bertorelli, Rosalia; Grilli, Mariagrazia; Lozza, Gianluca; Reggiani, Angelo; Li, Cheng.
Affiliation
  • Brumfield S; Merck Research Laboratories, 2015 Galloping Hill Road, MS 2545, Kenilworth, NJ 07033-0539, USA. Stephanie.Brumfield@merck.com
Bioorg Med Chem Lett ; 22(23): 7223-6, 2012 Dec 01.
Article in En | MEDLINE | ID: mdl-23084894
ABSTRACT
High throughput screening identified the pyridothienopyrimidinone 1 as a ligand for the metabotropic glutamate receptor 1 (mGluR1=10 nM). Compound 1 has an excellent in vivo profile; however, it displays unfavorable pharmacokinetic issues and metabolic stability. Therefore, using 1 as a template, novel analogues (10i) were prepared. These analogues displayed improved oral exposure and activity in the Spinal Nerve Ligation (SNL) pain model.
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidinones / Thiophenes / Receptors, Metabotropic Glutamate / Heterocyclic Compounds, 3-Ring Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Type: Article Affiliation country: United States
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Full text: 1 Collection: 01-internacional Database: MEDLINE Main subject: Pyrimidinones / Thiophenes / Receptors, Metabotropic Glutamate / Heterocyclic Compounds, 3-Ring Limits: Animals / Humans Language: En Journal: Bioorg Med Chem Lett Journal subject: BIOQUIMICA / QUIMICA Year: 2012 Type: Article Affiliation country: United States