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 ,
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
