Title of article
Structure–activity relationships of novel non-competitive mGluR1 antagonists: A potential treatment for chronic pain
Author/Authors
Dafydd R. Owen، نويسنده , , Peter G. Dodd، نويسنده , , Simon Gayton، نويسنده , , Ben S. Greener، نويسنده , , Gareth W. Harbottle، نويسنده , , Simon J. Mantell، نويسنده , , Graham N. Maw، نويسنده , , Simon A. Osborne، نويسنده , , Huw Rees، نويسنده , , Tracy J. Ringer، نويسنده , , Margarita Rodriguez-Lens، نويسنده , , Graham F. Smith، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2007
Pages
5
From page
486
To page
490
Abstract
A series of novel mGluR1 antagonists have been prepared. Incorporation of fragments derived from weak lead matter into a library led to enhanced potency in a new chemical series. A chemistry driven second library iteration, covering a greatly enhanced area of chemical space, maintained good potency and introduced metabolic stability.
Keywords
C log P , Log D , Quinoxaline , mGluR , pyrazine , mGluR1 , metabolism , library , CNS , Chronic pain
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2007
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
797681
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