2. Academic Validation
  3. Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam()

Synthesis and Evaluation of Metabotropic Glutamate Receptor Subtype 5 Antagonists Based on Fenobam()

  • ACS Med Chem Lett. 2011 Dec 8;2(12):882-884. doi: 10.1021/ml200162f.
Moses G Gichinga 1,  Jeremy P Olson,  Elizabeth Butala,  Hernán A Navarro,  Brian P Gilmour,  S Wayne Mascarella,  F Ivy Carroll
Affiliations

Affiliation

  • 1 Center for Organic and Medicinal Chemistry, Research Triangle Institute, Post Office Box 12194, Research Triangle Park, North Carolina 27709.
PMID: 22523618 DOI: 10.1021/ml200162f
Abstract

In an effort to discover potent and selective metabotropic glutamate receptor subtype 5 (mGluR5) antagonists, 15 tetrahydropyrimidinone analogues of 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-4,5-dihydro-1H-imidazol-2-yl)-urea (fenobam) were synthesized. These compounds were evaluated for antagonism of glutamate-mediated mobilization of internal calcium in an mGluR5 in vitro efficacy assay. The IC(50) value for 1-(3-chlorophenyl)-3-(1-methyl-4-oxo-1,4,5,6-tetrahydropyridine)urea (4g) was essentially identical to that of fenobam.

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