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Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists |
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| Authors: | 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 |
| Institution: | Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. Jared.Milbank@Pfizer.com |
| 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. |
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