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.

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

FILOSA, Rosanna;
2006

Abstract

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.
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/11591/335042
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