Abstract
Investigation of a series of heterobicyclic compounds with essential pharmacophoric features of the metabotropic glutamate receptor 5 (mGluR5) antagonists MPEP and MTEP provided novel structural templates with sub-micromolar affinities at the mGluR5.
Publication types
-
Research Support, N.I.H., Extramural
MeSH terms
-
Bridged Bicyclo Compounds, Heterocyclic / chemical synthesis
-
Bridged Bicyclo Compounds, Heterocyclic / chemistry*
-
Bridged Bicyclo Compounds, Heterocyclic / pharmacology*
-
Humans
-
Hydrolysis
-
Pyridines / chemistry*
-
Pyridines / pharmacology
-
Receptor, Metabotropic Glutamate 5
-
Receptors, Metabotropic Glutamate / antagonists & inhibitors*
-
Receptors, Metabotropic Glutamate / chemistry
-
Structure-Activity Relationship
-
Thiazoles / chemistry*
-
Thiazoles / pharmacology
Substances
-
3-((2-methyl-1,3-thiazol-4-yl)ethynyl)pyridine
-
Bridged Bicyclo Compounds, Heterocyclic
-
GRM5 protein, human
-
Pyridines
-
Receptor, Metabotropic Glutamate 5
-
Receptors, Metabotropic Glutamate
-
Thiazoles
-
6-methyl-2-(phenylethynyl)pyridine