Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists

Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.

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Bibliographische Detailangaben
Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2007-08, Vol.17 (16), p.4415-4418
Hauptverfasser:	Milbank, Jared B.J., Knauer, Christopher S., Augelli-Szafran, Corinne E., Sakkab-Tan, Annette T., Lin, Kristin K., Yamagata, Koji, Hoffman, Jennifer K., Zhuang, Nian, Thomas, John, Galatsis, Paul, Wendt, John A., Mickelson, John W., Schwarz, Roy D., Kinsora, Jack J., Lotarski, Susan M., Stakich, Korana, Gillespie, Kristen K., Lam, Wing W., Mutlib, Abdul E.
Format:	Artikel
Sprache:	eng
Schlagworte:	Antagonist Biological and medical sciences Drug Design Excitatory Amino Acid Antagonists - chemistry Excitatory Amino Acid Antagonists - pharmacology Glutamatergic system (aspartate and other excitatory aminoacids) Medical sciences mGluR5 Models, Molecular Molecular Structure MPEP Neuropharmacology Neurotransmitters. Neurotransmission. Receptors Pharmacology. Drug treatments Pyridines - chemistry Pyridines - pharmacology Quinolines - chemistry Quinolines - pharmacology Receptor, Metabotropic Glutamate 5 Receptors, Metabotropic Glutamate - antagonists & inhibitors Structure-Activity Relationship
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Beschreibung
Zusammenfassung:	Rational replacement of the alkyne linker of mGluR5 antagonist MPEP gave 7-arylquinolines. SAR optimization gave an orally active compound with high affinity for the MPEP binding site.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/j.bmcl.2007.06.030