2. Academic Validation
  3. Synthesis of heterocyclic enol ethers and their use as group 2 metabotropic glutamate receptor antagonists

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

  • Bioorg Med Chem Lett. 1999 Aug 2;9(15):2173-6. doi: 10.1016/s0960-894x(99)00346-7.
S Kolczewski 1,  G Adam,  H Stadler,  V Mutel,  J Wichmann,  T Woltering
Affiliations

Affiliation

  • 1 Pharma Division, Preclinical CNS Research, F. Hoffmann-La Roche Ltd., Basel. [email protected]
PMID: 10465539 DOI: 10.1016/s0960-894x(99)00346-7
Abstract

Heterocyclic enol ethers of type 1 were studied with respect to the inhibition of 1S,3R-ACPD (10 microM)-stimulated GTP gamma35S 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.

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