The discovery of potent, selective, and orally active pyrazoloquinolines as PDE10A inhibitors for the treatment of Schizophrenia

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 2, 2012, Pages 1019-1022

  Ho, Ginny D ^a   Yang, Shu Wei ^a   Smotryski, Jennifer ^a   Bercovici, Ana ^a   Nechuta, Terry ^a   Smith, Elizabeth M ^a   McElroy, William ^a   Tan, Zheng ^a   Tulshian, Deen ^a   McKittrick, Brian ^a   Greenlee, William J ^a   Hruza, Alan ^a   Xiao, Li ^a   Rindgen, Diane ^a   Mullins, Deborra ^a   Guzzi, Mario ^a   Zhang, Xiaoping ^a   Bleickardt, Carina ^a   Hodgson, Robert ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

PDE10A; Phosphodieasterase inhibitors; Schizophrenia

Indexed keywords

DIZOCILPINE; NEUROLEPTIC AGENT; PHOSPHODIESTERASE; PHOSPHODIESTERASE 10A; PYRAZOLOQUINOLINE DERIVATIVE; QUINOLINE DERIVATIVE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; ARTICLE; CONTROLLED STUDY; DRUG STRUCTURE; ENZYME INHIBITION; HIGH THROUGHPUT SCREENING; HYPERACTIVITY; LOCOMOTION; MOTOR DYSFUNCTION; NONHUMAN; RAT; SCHIZOPHRENIA; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; CRYSTALLOGRAPHY, X-RAY; DIZOCILPINE MALEATE; DOSE-RESPONSE RELATIONSHIP, DRUG; ENZYME INHIBITORS; HIGH-THROUGHPUT SCREENING ASSAYS; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PHOSPHORIC DIESTER HYDROLASES; PYRAZOLONES; QUINOLINES; RATS; SCHIZOPHRENIA; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84855681654     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.127     Document Type: Article

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