Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists

Heterocyclic enol ethers of type 1 were studied with respect to the inhibition of 1S,3R-ACPD (10μM)-stimulated GTP γ35S binding on rat mGluR2 transfected cell membranes. The structure activity relationship with regard to the substitution pattern of the phenyl ring, the oxygen substituent and the nature of the heterocycle is discussed.