875455-55-3Relevant academic research and scientific papers
Allosteric potentiators of the metabotropic glutamate receptor 2 (mGlu2). Part 2: 4-Thiopyridyl acetophenones as non-tetrazole containing mGlu2 receptor potentiators
Pinkerton, Anthony B.,Cube, Rowena V.,Hutchinson, John H.,James, Joyce K.,Gardner, Michael F.,Schaffhauser, Hervé,Rowe, Blake A.,Daggett, Lorrie P.,Vernier, Jean-Michel
, p. 5867 - 5872 (2007/10/03)
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. 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.
