Optimization of Novel Aza-benzimidazolone mGluR2 PAMs with Respect to LLE and PK Properties and Mitigation of CYP TDI

ACS Medicinal Chemistry Letters

Volumn 7, Issue 3, 2016, Pages 312-317

  Pero, Joseph E ^a,h   Rossi, Michael A ^a   Kelly, Michael J ^a   Lehman, Hannah D G F ^a   Layton, Mark E ^a   Garbaccio, Robert M ^a   O'Brien, Julie A ^b   Magliaro, Brian C ^c   Uslaner, Jason M ^d   Huszar, Sarah L ^d   Fillgrove, Kerry L ^e   Tang, Cuyue ^e   Kuo, Yuhsin ^e   Joyce, Leo A ^f   Sherer, Edward C ^g   Jacobson, Marlene A ^c  

^a Medicinal Chemistry   (United States)

^b Departments of in Vitro Pharmacology   (United States)

^c Psychiatry Research   (United States)

^d Central Pharmacology   (United States)

^e Drug Metabolism Department   (United States)

^f Process and Analytical Chemistry   (United States)

^g MERCK RESEARCH LABORATORIES   (United States)

^h GLAXOSMITHKLINE   (United States)

Author keywords

metabotropic glutamate receptor; positive allosteric modulator; Schizophrenia; time dependent inhibition

Indexed keywords

AMINO AZA BENZIMIDAZOLONE DERIVATIVE; BENZIMIDAZOLE DERIVATIVE; CYTOCHROME P450; METABOTROPIC RECEPTOR 2; METABOTROPIC RECEPTOR 2 POSITIVE ALLOSTERIC MODULATOR; METABOTROPIC RECEPTOR AGONIST; NEUROLEPTIC AGENT; UNCLASSIFIED DRUG;

ALLOSTERISM; ARTICLE; CELL MEMBRANE PERMEABILITY; DRUG BIOAVAILABILITY; DRUG EFFICACY; DRUG POTENCY; DRUG SELECTIVITY; DRUG SYNTHESIS; EC50; IN VITRO STUDY; LIPOPHILICITY; LIVER MICROSOME; NONHUMAN; PHARMACOPHORE; PHYSICAL CHEMISTRY; PRIORITY JOURNAL; SCHIZOPHRENIA; TIME-DEPENDENT INHIBITION;

EID: 84960923328     PISSN: None     EISSN: 19485875     Source Type: Journal    
DOI: 10.1021/acsmedchemlett.5b00459     Document Type: Article

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