Synthesis and preliminary biological evaluation of 2 '-substituted 2-(3 '-carboxybicyclo[1.1.1]-pentyl)glycine derivatives as group I selective metabotropic glutamate receptor ligands

The first series of 2'-substituted 2-(3'-carboxybicyclo-[1.1.1]phentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthe-sized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to be competitive group 1 mGluR antagonists. These results are also discussed in light of docking studies with both the active (closed) and inactive (open) conformations of mGluR1