Discovery and SAR of a novel series of metabotropic glutamate receptor 5 positive allosteric modulators with high ligand efficiency

Bioorganic and Medicinal Chemistry Letters

Volumn 24, Issue 15, 2014, Pages 3641-3646

  Turlington, Mark ^a,b,c   Noetzel, Meredith J ^a,b   Bridges, Thomas M ^a,b   Vinson, Paige N ^a,b   Steckler, Thomas ^d   Lavreysen, Hilde ^d   Mackie, Claire ^d   Bartolomé Nebreda, José M ^d   Conde Ceide, Susana ^d   Tong, Han Min ^d   Macdonald, Gregor J ^d   Daniels, J Scott ^a,b   Jones, Carrie K ^a,b   Niswender, Colleen M ^a,b   Conn, P Jeffrey ^a,b   Lindsley, Craig W ^a,b,c   Stauffer, Shaun R ^a,b,c  

^a VANDERBILT UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b VANDERBILT UNIVERSITY MEDICAL CENTER   (United States)

^c VANDERBILT UNIVERSITY   (United States)

^d JANSSEN RESEARCH AND DEVELOPMENT   (Belgium)

Author keywords

Positive allosteric modulator (PAM)

Indexed keywords

2 (PHENOXYMETHYL) 6,7 DIHYROPYRAZOLO[1,5 ALPHA]PYRIDIN 4(5H) ONE; METABOTROPIC RECEPTOR 5; METABOTROPIC RECEPTOR AGONIST; UNCLASSIFIED DRUG; VU 0462054; 2 (PHENOXYMETHYL) 6,7 DIHYDROPYRAZOLO[1,5 A]PYRIDIN 4(5H) ONE; ALCOHOL DERIVATIVE; ETHER DERIVATIVE; KETONE; METABOTROPIC GLUTAMATE RECEPTOR 5 POSITIVE ALLOSTERIC MODULATOR; 2-(PHENOXYMETHYL)-6,7-DIHYDROPYRAZOLO(1,5-A)PYRIDIN-4(5H)-ONE; LIGAND; PIPERIDONE DERIVATIVE; PYRAZOLE DERIVATIVE;

AEROBIC METABOLISM; ALKYLATION; ALLOSTERISM; AMINATION; ANIMAL EXPERIMENT; ARTICLE; ARYLATION; BINDING SITE; DEBENZYLATION; DECARBOXYLATION; DRUG CLEARANCE; DRUG METABOLISM; DRUG POTENCY; DRUG PURIFICATION; DRUG SYNTHESIS; HYDROGEN BOND; IN VITRO STUDY; IN VIVO STUDY; LIVER BLOOD FLOW; LIVER CLEARANCE; MALE; METHYLATION; NONHUMAN; PHYSICAL CHEMISTRY; PLASMA PROTEIN BINDING; RAT; STRUCTURE ACTIVITY RELATION; TURNOVER TIME; EC50; HUMAN; PHARMACOPHORE; ANIMAL; CELL LINE; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG DEVELOPMENT; DRUG EFFECTS; METABOLISM; SYNTHESIS;

ALLOSTERIC REGULATION; ANIMALS; CELL LINE; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; HUMANS; LIGANDS; MOLECULAR STRUCTURE; PIPERIDONES; PYRAZOLES; RATS; RECEPTOR, METABOTROPIC GLUTAMATE 5; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84904038714     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2014.04.087     Document Type: Article

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