Application of structure-based drug design and parallel chemistry to identify selective, brain penetrant, in vivo active phosphodiesterase 9A inhibitors

Journal of Medicinal Chemistry

Volumn 55, Issue 21, 2012, Pages 9055-9068

  Claffey, Michelle M ^a   Helal, Christopher J ^a   Verhoest, Patrick R ^a   Kang, Zhijun ^a   Fors, Kristina S ^a   Jung, Stanley ^a   Zhong, Jiaying ^a   Bundesmann, Mark W ^a   Hou, Xinjun ^a   Lui, Shenping ^a   Kleiman, Robin J ^a   Vanase Frawley, Michelle ^a   Schmidt, Anne W ^a   Menniti, Frank ^a   Schmidt, Christopher J ^a   Hoffman, William E ^a   Hajos, Mihaly ^a   McDowell, Laura ^a   Oconnor, Rebecca E ^a   MacDougall Murphy, Mary ^a   Fonseca, Kari R ^a   Becker, Stacey L ^a   Nelson, Frederick R ^a   Liras, Spiros ^a   more..

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 CYCLOPENTYL 6 [1 (3 PYRIMIDIN 2 YLAZETIDIN 1 YL)ETHYL] 1,5 DIHYDRO 4H PYRAZOLO[3,4 D]PYRIMIDIN 4 ONE; CYCLIC GMP; PF 04447943; PHOSPHODIESTERASE; PHOSPHODIESTERASE 1C; PHOSPHODIESTERASE 9A; PHOSPHODIESTERASE 9A INHIBITOR; PHOSPHODIESTERASE INHIBITOR; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CEREBROSPINAL FLUID; CONTROLLED STUDY; CYTOTOXICITY; DOG; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG DESIGN; DRUG DISTRIBUTION; DRUG PENETRATION; DRUG POTENCY; DRUG SELECTIVITY; DRUG STRUCTURE; DRUG SYNTHESIS; ENZYME INHIBITION; HUMAN; IN VIVO STUDY; NONHUMAN; PHYSICAL CHEMISTRY; QT PROLONGATION; RAT; STRUCTURE ACTIVITY RELATION;

3',5'-CYCLIC-AMP PHOSPHODIESTERASES; ADMINISTRATION, ORAL; ANIMALS; AZETIDINES; BLOOD-BRAIN BARRIER; CRYSTALLOGRAPHY, X-RAY; CYCLIC GMP; CYCLOPENTANES; DATABASES, FACTUAL; DOGS; DRUG DESIGN; HUMANS; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PYRAZOLES; PYRIMIDINES; PYRIMIDINONES; RATS; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84868515345     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm3009635     Document Type: Article

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