Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides as potent, orally available mGlu1 receptor enhancers

Small molecule mGluR1 enhancers, which are 9H-xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides, have been previously reported. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides with improved pharmacokinetic properties have been designed and synthesized as us...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2009-03, Vol.19 (6), p.1666-1669
Hauptverfasser:	Vieira, Eric, Huwyler, Jörg, Jolidon, Synèse, Knoflach, Frédéric, Mutel, Vincent, Wichmann, Jürgen
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral Amides - chemistry Animals Chemistry, Pharmaceutical - methods CHO Cells Cricetinae Cricetulus Drug Design Electrophysiology - methods Humans Models, Chemical Molecular Structure Rats Receptors, Metabotropic Glutamate - chemistry Receptors, Metabotropic Glutamate - metabolism Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Small molecule mGluR1 enhancers, which are 9H-xanthene-9-carboxylic acid [1,2,4]oxadiazol-3-yl- and (2H-tetrazol-5-yl)-amides, have been previously reported. Fluorinated 9H-xanthene-9-carboxylic acid oxazol-2-yl-amides with improved pharmacokinetic properties have been designed and synthesized as useful pharmacological tools for the study of the physiological roles mediated by mGlu1 receptors. The synthesis and the structure-activity relationship of this class of positive allosteric modulators of mGlu1 receptors will be discussed in detail.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2009.01.108