2. Academic Validation
  3. Discovery of novel modulators of metabotropic glutamate receptor subtype-5

Discovery of novel modulators of metabotropic glutamate receptor subtype-5

  • Bioorg Med Chem. 2004 Jan 2;12(1):17-21. doi: 10.1016/j.bmc.2003.10.021.
Bowei Wang 1,  Jean Michel Vernier,  Sara Rao,  Janice Chung,  Jeffery J Anderson,  Jesse D Brodkin,  Xiaohui Jiang,  Michael F Gardner,  Xiaoqing Yang,  Benito Munoz
Affiliations

Affiliation

  • 1 Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, 92121, San Diego, CA 92121, USA. bowei_wang@merck.com
PMID: 14697765 DOI: 10.1016/j.bmc.2003.10.021
Abstract

A series of potent and selective mGluR5 antagonists were synthesized and evaluated in vitro and in vivo. It was found that a pyridyl functionality is a potential replacement for acetonitrile in the lead structure, with 2-pyridyl being most favored. Additionally, the benzoxazole moiety could also be replaced by Other heterobicyclic rings such as imidazothiazole.

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