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Metropolitan Government of Nashville-Davidson (balance), TN, United States

Reid P.R.,Vanderbilt Institute of Chemical Biology Chemical Synthesis Core | Bridges T.M.,Vanderbilt University | Bridges T.M.,Vanderbilt Specialized Chemistry Center | Sheffler D.J.,Vanderbilt University | And 20 more authors.
Bioorganic and Medicinal Chemistry Letters | Year: 2011

This Letter describes a chemical lead optimization campaign directed at VU0108370, a weak M1 PAM hit with a novel chemical scaffold from a functional HTS screen within the MLPCN. An iterative parallel synthesis approach rapidly established SAR for this series and afforded VU0405652 (ML169), a potent, selective and brain penetrant M1 PAM with an in vitro profile comparable to the prototypical M1 PAM, BQCA, but with an improved brain to plasma ratio. © 2010 Elsevier Ltd. All rights reserved. Source

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