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
  • 1. Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, 92121, San Diego, CA 92121, USA. [email protected]
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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