Discovery of orally active pyrazoloquinolines as potent PDE10 inhibitors for the management of schizophrenia

Bioorganic and Medicinal Chemistry Letters

Volumn 22, Issue 1, 2012, Pages 235-239

  Yang, Shu Wei ^a   Smotryski, Jennifer ^a   McElroy, William T ^a   Tan, Zheng ^a   Ho, Ginny ^a   Tulshian, Deen ^a   Greenlee, William J ^a   Guzzi, Mario ^a   Zhang, Xiaoping ^a   Mullins, Deborra ^a   Xiao, Li ^a   Hruza, Alan ^a   Chan, Tze Ming ^a   Rindgen, Diane ^a   Bleickardt, Carina ^a   Hodgson, Robert ^a  

^a MERCK RESEARCH LABORATORIES   (United States)

Author keywords

Antipsychotic; Inhibitors; PDE10; Pyrazoloquinoline; Schizophrenia

Indexed keywords

DIZOCILPINE; NEUROLEPTIC AGENT; PYRAZOLOQUINOLINE; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ANIMAL MODEL; AREA UNDER THE CURVE; ARTICLE; BINDING AFFINITY; DRUG BINDING; DRUG POTENCY; DRUG SYNTHESIS; NONHUMAN; RAT; SCHIZOPHRENIA; STRUCTURE ACTIVITY RELATION;

ADMINISTRATION, ORAL; ANIMALS; ANTIPSYCHOTIC AGENTS; CHEMISTRY, PHARMACEUTICAL; CRYSTALLOGRAPHY, X-RAY; DISEASE MODELS, ANIMAL; DIZOCILPINE MALEATE; DRUG DESIGN; EXCITATORY AMINO ACID ANTAGONISTS; HUMANS; MODELS, CHEMICAL; MOLECULAR CONFORMATION; PHOSPHODIESTERASE INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; PYRAZOLES; QUINOLINES; RATS; SCHIZOPHRENIA; STRUCTURE-ACTIVITY RELATIONSHIP;

RATTUS;

EID: 84655170136     PISSN: 0960894X     EISSN: 14643405     Source Type: Journal    
DOI: 10.1016/j.bmcl.2011.11.023     Document Type: Article

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