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. Research Abstract Details 

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Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Abstract Text:

Jared B J Milbank,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,

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.

Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Publishing Authors By Initials

JB Milbank,CS Knauer,CE Augelli-Szafran,AT Sakkab-Tan,KK Lin,K Yamagata,JK Hoffman,N Zhuang,J Thomas,P Galatsis,JA Wendt,JW Mickelson,RD Schwarz,JJ Kinsora,SM Lotarski,K Stakich,KK Gillespie,WW Lam,AE Mutlib,

For similar biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research abstracts see: biochemical phenomena, metabolism, and nutrition: biochemical phenomena: structure-activity relationship research

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Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Bioorganic & medicinal chemistry letters

VOLUME: 17

Page Numbers: 4415-8

Journal Abbreviation: Bioorg. Med. Chem. Lett.

ISSN: 0960-894X

DAY: 10

MONTH: 06

YEAR: 2007

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

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LANGUAGE: eng

NlmUniqueID: 9107377

Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Keywords Mesh Terms:

KEYWORDS: Structure-Activity Relationship

MESH TERMS: antagonists & inhibitors

Chemical & Substance for Abstract: Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists. Information

Substance Name: metabotropic glutamate receptor 5

Registry Number: 0

Grant and Affiliation Information for Rational design of 7-arylquinolines as non-competitive metabotropic glutamate receptor subtype 5 antagonists.

AFFILIATION: Pfizer Global Research and Development, Michigan Laboratories, 2800 Plymouth Road, Ann Arbor, MI 48105, USA. Jared.Milbank@Pfizer.com

Country: England

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MEDLINETA: Bioorg Med Chem Lett

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