Time filter

Source Type

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.


PubMed | Vanderbilt Institute of Chemical Biology Chemical Synthesis Core
Type: Journal Article | Journal: Bioorganic & medicinal chemistry letters | Year: 2011

This Letter describes a chemical lead optimization campaign directed at VU0108370, a weak M(1) 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 M(1) PAM with an in vitro profile comparable to the prototypical M(1) PAM, BQCA, but with an improved brain to plasma ratio.

Loading Vanderbilt Institute of Chemical Biology Chemical Synthesis Core collaborators
Loading Vanderbilt Institute of Chemical Biology Chemical Synthesis Core collaborators