2. Academic Validation
  3. Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists

Design and synthesis of noncompetitive metabotropic glutamate receptor subtype 5 antagonists

  • Bioorg Med Chem Lett. 2006 Jul 1;16(13):3371-5. doi: 10.1016/j.bmcl.2006.04.032.
Santosh S Kulkarni 1,  Barbara Nightingale,  Christina M Dersch,  Richard B Rothman,  Amy Hauck Newman
Affiliations

Affiliation

  • 1 Medicinal Chemistry Section, National Institute on Drug Abuse, Intramural Research Program, NIH, DHHS, 5500 Nathan Shock Drive, Baltimore, MD 21224, USA.
PMID: 16678408 DOI: 10.1016/j.bmcl.2006.04.032
Abstract

A series of diaryl amides was designed and synthesized as novel nonethynyl mGluR5 antagonists. The systematic variation of the pharmacophoric groups led to the identification of a lead compound that demonstrated micromolar affinity for the mGluR5. Further optimization resulted in compounds with improved binding affinities and antagonist profiles, in vitro.

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