Synthesis and SAR study of new phenylimidazole-pyrazolo[1,5-c]quinazolines as potent phosphodiesterase 10A inhibitors

Bioorganic and Medicinal Chemistry

Volumn 19, Issue 1, 2011, Pages 642-649

  Asproni, Battistina ^a   Murineddu, Gabriele ^a   Pau, Amedeo ^a   Pinna, Gérard A ^a   Langgård, Morten ^b   Christoffersen, Claus Tornby ^b   Nielsen, Jacob ^b   Kehler, Jan ^b  

^a UNIVERSITY OF SASSARI   (Italy)

^b H LUNDBECK A S   (Denmark)

Author keywords

PDE10A inhibition; Phenylimidazole pyrazolo 1,5 c quinazolines; Structure activity relationships

Indexed keywords

2 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 2 CHLORO 6 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 2 METHOXY 6 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 2 METHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO) METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 2 METHYL 6 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 2,7 DIMETHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 2,9 DIMETHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 4 CHLORO 2 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 4 METHOXY 2 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 4 METHYL 2 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 5 (CHLOROMETHYL) 2 METHYLPYRAZOLO[1,5 C]QUINAZOLINE; 5 (CHLOROMETHYL) 2,7 DIMETHYLPYRAZOLO[1,5 C]QUINAZOLINE; 5 (CHLOROMETHYL) 2,9 DIMETHYLPYRAZOLO[1,5 C]QUINAZOLINE; 5 (CHLOROMETHYL) 7 METHOXY 2 METHYLPYRAZOLO[1,5 C] QUINAZOLINE; 5 (CHLOROMETHYL) 8 METHOXY 2 METHYLPYRAZOLO[1,5 C] QUINAZOLINE; 5 (CHLOROMETHYL) 9 METHOXY 2 METHYLPYRAZOLO[1,5 C] QUINAZOLINE; 5 CHLORO 2 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 5 METHOXY 2 (3 METHYL 1H PYRAZOL 5 YL)ANILINE; 7 CHLORO 2 METHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 7 CHLORO 5 (CHLOROMETHYL) 2 METHYLPYRAZOLO[1,5 C]QUINAZOLINE; 7 METHOXY 2 METHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 8 CHLORO 2 METHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 8 CHLORO 5 (CHLOROMETHYL) 2 METHYLPYRAZOLO[1,5 C]QUINAZOLINE; 8 METHOXY 2 METHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 9 CHLORO 2 METHYL 5 [(1 METHYL 4 PHENYL 1H IMIDAZOL 2 YLTHIO)METHYL]PYRAZOLO[1,5 C]QUINAZOLINE; 9 CHLORO 5 (CHLOROMETHYL) 2 METHYLPYRAZOLO[1,5 C]QUINAZOLINE; PHENYLIMIDAZOLE PYRAZOLO[1,5 C]QUINAZOLINE; PHOSPHODIESTERASE INHIBITOR; QUINAZOLINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ARTICLE; BINDING AFFINITY; DRUG BINDING; DRUG SYNTHESIS; IC 50;

ANIMALS; BLOOD-BRAIN BARRIER; INHIBITORY CONCENTRATION 50; MAGNETIC RESONANCE SPECTROSCOPY; MASS SPECTROMETRY; MICE; MODELS, MOLECULAR; PHOSPHODIESTERASE INHIBITORS; PHOSPHORIC DIESTER HYDROLASES; QUINAZOLINES; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 78650751009     PISSN: 09680896     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.bmc.2010.10.038     Document Type: Article

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