Discovery of molecular switches within the ADX-47273 mGlu sub(5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu) sub(5) NAMs, PAMs and partial antagonists

Discovery of molecular switches within the ADX-47273 mGlu sub(5 PAM scaffold that modulate modes of pharmacology to afford potent mGlu) sub(5) NAMs, PAMs and partial antagonists

This Letter describes a chemical lead optimization campaign directed at a weak mGlu sub(5 NAM discovered while developing SAR for the mGlu) sub(5) PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu sub(5 NAMs, mGlu) sub(5) PA...

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters Vol. 21; no. 9; pp. 2711 - 2714
Main Authors: Lamb, Jeffrey P, Engers, Darren W, Niswender, Colleen M, Rodriguez, Alice L, Venable, Daryl F, Conn, Jeffrey P, Lindsley, Craig W
Format: Journal Article
Language:English
Published: 01-05-2011
Online Access:Get full text
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Summary:This Letter describes a chemical lead optimization campaign directed at a weak mGlu sub(5 NAM discovered while developing SAR for the mGlu) sub(5) PAM, ADX-47273. An iterative parallel synthesis effort discovered multiple, subtle molecular switches that afford potent mGlu sub(5 NAMs, mGlu) sub(5) PAMs as well as mGlu sub(5 partial antagonists.)
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SourceType-Scholarly Journals-1
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2010.11.119