| Literature DB >> 16439120 |
Bernd Büttelmann1, Jens-Uwe Peters, Simona Ceccarelli, Sabine Kolczewski, Eric Vieira, Eric P Prinssen, Will Spooren, Franz Schuler, Jörg Huwyler, Richard H P Porter, Georg Jaeschke.
Abstract
Optimisation of affinity, chemical stability, metabolic stability and solubility led from a chemically labile HTS hit 1 to mGlu5 receptor antagonists (24-26) with high affinity for the allosteric MPEP binding site, improved microsomal metabolic stability and anxiolytic-like activity in vivo as assessed by the Vogel conflict drinking test.Entities:
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Year: 2006 PMID： 16439120 DOI： 10.1016/j.bmcl.2005.12.088
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823