Title of article
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-Thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators
Author/Authors
Anthony B. Pinkerton، نويسنده , , Rowena V. Cube، نويسنده , , John H. Hutchinson، نويسنده , , Joyce K. James، نويسنده , , Michael F. Gardner، نويسنده , , Herve Schaffhauser، نويسنده , , Blake A. Rowe، نويسنده , , Lorrie P. Daggett، نويسنده , , Jean-Michel Vernier، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2004
Pages
6
From page
5867
To page
5872
Abstract
We have identified and synthesized a series of 4-thiopyridyl acetophenones as positive allosteric potentiators of the metabotropic glutamate receptor 2. Structure–activity relationship studies directed toward replacement of the tetrazole in the initial lead led to the discovery of 16 (EC50 = 340 nM), which showed improved brain penetration over the initial lead.
Keywords
e-mail: anthony_pinkerton@merck.com , fax: +1 858 202 5752 , Allosteric.* Corresponding author. Tel.: +1 858 202 5379 , Glutamate receptors , GPCRs , Schizophrenia
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2004
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
795085
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