Discovery and structure-activity relationship of 1,3-cyclohexyl amide derivatives as novel mGluR5 negative allosteric modulators

Bioorganic and Medicinal Chemistry Letters

Volumn 23, Issue 5, 2013, Pages 1398-1406

  Zhou, Hao ^a   Topiol, Sidney W ^a,c   Grenon, Michel ^a   Jimenez, Hermogenes N ^a   Uberti, Michelle A ^a   Smith, Daniel G ^a   Brodbeck, Robbin M ^a   Chandrasena, Gamini ^a   Pedersen, Henrik ^b   Madsen, Jens Christian ^b,d   Doller, Darío ^a   Li, Guiying ^a  

^a LUNDBECK RESEARCH USA   (United States)

^b H LUNDBECK A S   (Denmark)

^c 3D 2drug ^*  (United States)

^d Bruker Corporation   (United States)

Author keywords

mGluR5; Negative allosteric modulator

Indexed keywords

1,3 CYCLOHEXYL AMIDE DERIVATIVE; ANXIOLYTIC AGENT; METABOTROPIC RECEPTOR 5; UNCLASSIFIED DRUG;

ALLOSTERISM; AMIDATION; ANIMAL EXPERIMENT; ARTICLE; CELL STRAIN HEK293; CENTRAL NERVOUS SYSTEM; DRUG PENETRATION; DRUG POTENCY; DRUG STRUCTURE; HETERONUCLEAR SINGLE QUANTUM COHERENCE; IN VITRO STUDY; MALE; MOUSE; NONHUMAN; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION; TRANQUILIZING ACTIVITY;

ALLOSTERIC REGULATION; AMIDES; ANIMALS; CYCLOHEXANES; HEK293 CELLS; HUMANS; MICE; MODELS, MOLECULAR; MOLECULAR CONFORMATION; RECEPTOR, METABOTROPIC GLUTAMATE 5; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84873729569     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.12.078     Document Type: Article

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