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VU6010608, a Novel mGlu7 NAM from a Series of N-(2-(1H-1,2,4-Triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamides.
Reed, Carson W; McGowan, Kevin M; Spearing, Paul K; Stansley, Branden J; Roenfanz, Hanna F; Engers, Darren W; Rodriguez, Alice L; Engelberg, Eileen M; Luscombe, Vincent B; Loch, Matthew T; Remke, Daniel H; Rook, Jerri M; Blobaum, Anna L; Conn, P Jeffrey; Niswender, Colleen M; Lindsley, Craig W.
Afiliação
  • Reed CW; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • McGowan KM; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Spearing PK; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Stansley BJ; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Roenfanz HF; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Engers DW; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Rodriguez AL; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Engelberg EM; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Luscombe VB; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Loch MT; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Remke DH; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Rook JM; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Blobaum AL; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Conn PJ; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
  • Niswender CM; Vanderbilt Kennedy Center, Vanderbilt University Medical Center, Nashville, Tennessee 37232, United States.
  • Lindsley CW; Vanderbilt Center for Neuroscience Drug Discovery, Department of Pharmacology, and Department of Biochemistry and Chemistry, Vanderbilt University, Nashville, Tennessee 37232, United States.
ACS Med Chem Lett ; 8(12): 1326-1330, 2017 Dec 14.
Article em En | MEDLINE | ID: mdl-29259756
ABSTRACT
Herein, we report the structure-activity relationships within a series of mGlu7 NAMs based on an N-(2-(1H-1,2,4-triazol-1-yl)-5-(trifluoromethoxy)phenyl)benzamide core with excellent CNS penetration (Kp 1.9-5.8 and Kp,uu 0.4-1.4). Analogues in this series displayed steep SAR. Of these, VU6010608 (11a) emerged with robust efficacy in blocking high frequency stimulated long-term potentiation in electrophysiology studies.
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Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos
Texto completo
Imprimir
XML
PubMed Links
Buscar no Google

Texto completo: 1 Base de dados: MEDLINE Idioma: En Revista: ACS Med Chem Lett Ano de publicação: 2017 Tipo de documento: Article País de afiliação: Estados Unidos