Abstract
The first series of 2'-substituted 2-(3'-carboxybicyclo[1.1.1]pentyl)glycine derivatives, (2R)- and (2S)-(2',2'-dichloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (10) and (11), and 2-(2'-chloro-3'-carboxybicyclo[1.1.1]pentyl)glycine (12) were synthesized and evaluated as mGluR ligands. Compounds 11 and 12 were shown to be competitive group I mGluR antagonists. These results are also discussed in light of docking studies with both the active (closed) and inactive (open) conformations of mGluR1.
MeSH terms
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Bridged Bicyclo Compounds / chemical synthesis*
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Bridged Bicyclo Compounds / metabolism
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Bridged Bicyclo Compounds / pharmacology*
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Glycine / analogs & derivatives*
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Glycine / chemical synthesis
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Glycine / metabolism
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Glycine / pharmacology
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Ligands
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Magnetic Resonance Spectroscopy
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Models, Molecular
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Receptors, Metabotropic Glutamate / drug effects*
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Receptors, Metabotropic Glutamate / metabolism
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Structure-Activity Relationship
Substances
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Bridged Bicyclo Compounds
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Ligands
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Receptors, Metabotropic Glutamate
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UPF 596
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Glycine