Discovery of a novel class of phosphodiesterase 10A inhibitors and identification of clinical candidate 2-[4-(1-methyl-4-pyridin-4-yl-1H-pyrazol-3- yl)-phenoxymethyl]-quinoline (PF-2545920) for the treatment of schizophrenia

Journal of Medicinal Chemistry

Volumn 52, Issue 16, 2009, Pages 5188-5196

  Verhoest, Patrick R ^a   Chapin, Douglas S ^a   Corman, Michael ^a   Fonseca, Kari ^a   Harms, John F ^a   Hou, Xinjun ^a   Marr, Eric S ^a   Menniti, Frank S ^a   Nelson, Frederick ^a   O'Connor, Rebecca ^a   Pandit, Jayvardhan ^a   Proulx LaFrance, Caroline ^a   Schmidt, Anne W ^a   Schmidt, Christopher J ^a   Suiciak, Judith A ^a   Liras, Spiros ^a  

^a PFIZER INC   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

1 (4 BENZYLOXYPHENYL) 2 PYRIDIN 4 YLETHANONE; 1 METHYL 2 [4 (1 METHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOXYMETHYL]1H BENZOIMIDAZOLE; 2 [4 (1 ETHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (1 METHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOXYMETHYL][1,2,4]TRIAZOLO[1,5 A]PYRIDINE; 2 [4 (1 METHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOXYMETHYL]IMIDAZO[1,2 A]PYRIDINE; 2 [4 (1 METHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (1 METHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOXALINE; 2 [4 (2 ETHYL 4 PYRIDIN 4 YL 2H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (2 METHYL 4 PYRIDIN 4 YL 2H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (2 METHYL 5 PYRIDIN 4 YLPYRIMIDIN 4 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (4 PYRIDAZIN 4 YL 2H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (4 PYRIDIN 4 YL 2H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (4 PYRIDIN 4 YLISOXAZOL 5 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 (4 PYRIMIDIN 4 YL 2H PYRAZOL 3 YL)PHENOXYMETHYL]QUINOLINE; 2 [4 [4 (3 METHYLISOXAZOL 5 YL) 2H PYRAZOL 3 YL]PHENOXYMETHYL]QUINOLINE; 2 [4 [PYRIDIN 4 YL 1 (2,2,2 TRIFLUOROETHYL) 1H PYRAZOL 3 YL]PHENOXYMETHYL]QUINOLINE; 2 [[4 (4 PHENYL 1H PYRAZOL 5 YL)PHENOXY]METHYL]QUINOLINE; 2 [[4 [4 (PYRIDIN 2 YL) 1H PYRAZOL 5 YL]PHENOXY]METHYL]QUINOLINE; 2 PYRIDIN 4 YL 1 [4 (QUINOLIN 2 YLMETHOXY)PHENYL]ETHANONE; 3 DIMETHYLAMINO 2 PYRIDIN 4 YL 1 [4 (QUINOLIN 2 YLMETHOXY)PHENYL]PROPENONE; 4 (1 METHYL 4 PYRIDIN 4 YL 1H PYRAZOL 3 YL)PHENOL; 4 (QUINOLIN 2 YLMETHOXY)BENZOIC ACID; 4 [3 (4 BENZYLOXYPHENYL) 1 METHYL 1H PYRAZOL 4 YL]PYRIDINE; 4 BENZYLOXY N METHOXY N METHYLBENZAMIDE; N METHOXY N METHYL 4 (QUINOLIN 2 YLMETHOXY)BENZAMIDE; PF 2545920; PHOSPHODIESTERASE; PHOSPHODIESTERASE INHIBITOR; PHOSPHODIESTERASE XA INHIBITOR; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; DISTRIBUTION VOLUME; DOSE RESPONSE; DRUG BINDING SITE; DRUG CLEARANCE; DRUG DESIGN; DRUG HALF LIFE; DRUG IDENTIFICATION; DRUG MECHANISM; DRUG PENETRATION; DRUG POTENCY; DRUG PROTEIN BINDING; DRUG SAFETY; DRUG SCREENING; DRUG SELECTIVITY; ENZYME INHIBITION; HYDROGEN BOND; IC 50; MOUSE; NONHUMAN; RAT; SCHIZOPHRENIA; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ANIMALS; ANTIPSYCHOTIC AGENTS; AVOIDANCE LEARNING; BINDING SITES; BRAIN; CRYSTALLOGRAPHY, X-RAY; DOGS; FEMALE; HUMANS; HYDROGEN BONDING; MACACA FASCICULARIS; MALE; MICE; MICE, KNOCKOUT; MICROSOMES, LIVER; MODELS, MOLECULAR; MOLECULAR STRUCTURE; PHOSPHORIC DIESTER HYDROLASES; PROTEIN BINDING; PYRAZOLES; QUINOLINES; RATS; RATS, SPRAGUE-DAWLEY; SCHIZOPHRENIA; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 69049103114     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm900521k     Document Type: Article

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