| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1374347 | Bioorganic & Medicinal Chemistry Letters | 2011 | 4 Pages |
Abstract
This Letter describes a chemical lead optimization campaign directed at a weak mGlu5 NAM discovered while developing SAR for the mGlu5 PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu5 NAMs, mGlu5 PAMs as well as mGlu5 partial antagonists.
Graphical abstractThis Letter describes a chemical lead optimization campaign directed at a weak mGlu5 NAM discovered while developing SAR for the mGlu5 PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu5 NAMs, mGlu5 PAMs as well as mGlu5 partial antagonists.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Jeffrey P. Lamb, Darren W. Engers, Colleen M. Niswender, Alice L. Rodriguez, Daryl F. Venable, P. Jeffrey Conn, Craig W. Lindsley,