| Literature DB >> 15482907 |
Steve F Poon1, Brian W Eastman, Deborah F Chapman, Janice Chung, Merryl Cramer, Gregory Holtz, Nicholas D P Cosford, Nicholas D Smith.
Abstract
Structure-activity relationship studies performed around 3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)benzonitrile for the purpose of developing novel mGlu5 receptor antagonists are described. Synthesis of a series of four-ring tetrazoles led to the discovery of 3-[3-fluoro-5-(5-pyridin-2-yl-2H-tetrazol-2-yl)phenyl]-4-methylpyridine, a highly potent, brain penetrant, azole-based mGlu5 receptor antagonist.Entities:
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Year: 2004 PMID： 15482907 DOI： 10.1016/j.bmcl.2004.09.011
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823