Discovery of potent, selective, and metabolically stable 4-(pyridin-3-yl)cinnolines as novel phosphodiesterase 10A (PDE10A) inhibitors

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 6, 2012, Pages 2262-2265

  Hu, Essa ^a   Kunz, Roxanne K ^a   Rumfelt, Shannon ^a   Chen, Ning ^a   Bürli, Roland ^b   Li, Chun ^d   Andrews, Kristin L ^a   Zhang, Jiandong ^a   Chmait, Samer ^a   Kogan, Jeffrey ^e   Lindstrom, Michelle ^a   Hitchcock, Stephen A ^a,c   Treanor, James ^a  

^a AMGEN INC   (United States)

^b BioFocus DPI   (United Kingdom)

^c Envoy Therapeutics   (United States)

^d GENOMICS INSTITUTE OF THE NOVARTIS RESEARCH FOUNDATION   (United States)

^e ASTELLAS PHARMA GLOBAL DEVELOPMENT   (United States)

Author keywords

Cinnolines; Metabolism; PDE10A; Phosphodiesterase; Schizophrenia

Indexed keywords

4 (PYRIDIN 3 YL)CINNOLINE DERIVATIVE; PHOSPHODIESTERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CRYSTAL STRUCTURE; DRUG CLEARANCE; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; ENZYME DEGRADATION; IN VIVO STUDY; NONHUMAN; RAT; SCHIZOPHRENIA; STRUCTURE ACTIVITY RELATION; X RAY ANALYSIS;

ANIMALS; AVOIDANCE LEARNING; BEHAVIOR, ANIMAL; BINDING SITES; COUMARINS; DRUG DISCOVERY; HUMANS; MODELS, MOLECULAR; PHOSPHODIESTERASE INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; PROTEIN BINDING; PSYCHOTROPIC DRUGS; RATS; RATS, SPRAGUE-DAWLEY; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS; RODENTIA;

EID: 84862811342     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2012.01.086     Document Type: Article

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