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

descriptionPublicationkeyboard_double_arrow_right Article 01 Aug 2007Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 17, pages 4,415-4,418 (issn: 0960-894X,

Authors: Kristen K. Gillespie; John A. Wendt; Jared B.J. Milbank; Corinne E. Augelli-Szafran; Susan M. Lotarski; Annette T. Sakkab-Tan; Jack J. Kinsora; +12 Authors

doi: 10.1016/j.bmcl.2007.06.030

pmid: 17590335

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

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Abstract

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.

Related Organizations

Pfizer (United States)
United States

Keywords

Models, Molecular, Structure-Activity Relationship, Molecular Structure, Pyridines, Drug Design, Receptor, Metabotropic Glutamate 5, Quinolines, Receptors, Metabotropic Glutamate, Excitatory Amino Acid Antagonists

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BindingDB Entry 50020706: Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.
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