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Synthesis and evaluation of a series of heterobiarylamides that are centrally penetrant metabotropic glutamate receptor 4 (mGluR4) positive allosteric modulators (PAMs).


AUTHORS

Engers DWDarren W , Niswender CM Colleen M , Weaver CD C David , Jadhav S Satyawan , Menon UN Usha N , Zamorano R Rocio , Conn PJ P Jeffrey , Lindsley CW Craig W , Hopkins CR Corey R . Journal of medicinal chemistry. 2009 7 23; 52(14). 4115-8

ABSTRACT

We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.


We report the synthesis and evaluation of a series of heterobiaryl amides as positive allosteric modulators of mGluR4. Compounds 9b and 9c showed submicromolar potency at both human and rat mGluR4. In addition, both 9b and 9c were shown to be centrally penetrant in rats using nontoxic vehicles, a major advance for the mGluR4 field.