1. Academic Validation
  2. Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists

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

  • Bioorg Med Chem Lett. 2007 Aug 15;17(16):4415-8. doi: 10.1016/j.bmcl.2007.06.030.
Jared B J Milbank 1 Christopher S Knauer Corinne E Augelli-Szafran Annette T Sakkab-Tan Kristin K Lin Koji Yamagata Jennifer K Hoffman Nian Zhuang John Thomas Paul Galatsis John A Wendt John W Mickelson Roy D Schwarz Jack J Kinsora Susan M Lotarski Korana Stakich Kristen K Gillespie Wing W Lam Abdul E Mutlib
Affiliations

Affiliation

  • 1 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.

Figures