Discovery of novel modulators of metabotropic glutamate receptor subtype-5 |
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| Authors: | Wang Bowei Vernier Jean Michel Rao Sara Chung Janice Anderson Jeffery J Brodkin Jesse D Jiang Xiaohui Gardner Michael F Yang Xiaoqing Munoz Benito |
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| Affiliation: | Department of Chemistry, Merck Research Laboratories, MRLSDB2, 3535 General Atomics Court, 92121, San Diego, CA 92121, USA. bowei_wang@merck.com |
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| 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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