Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists
A series of diaryl amides was designed and synthesized as novel nonethynyl mGluR5 antagonists. The systematic variation of the pharmacophoric groups led to the identification of a lead compound that demonstrated micromolar affinity for the mGluR5. Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro.
Kulkarni, Santosh S.,Nightingale, Barbara,Dersch, Christina M.,Rothman, Richard B.,Newman, Amy Hauck
p. 3371 - 3375
(2007/10/03)
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