Triazolyl azabicyclo[3.1.0]hexanes: A class of potent and selective dopamine D3 receptor antagonists

ChemMedChem

Volumn 5, Issue 5, 2010, Pages 705-715

  Bonanomi, Giorgio ^a   Braggio, Simone ^a   Capelli, Anna Maria ^a   Checchia, Anna ^a   Di Fabio, Romano ^a   Marchioro, Carla ^a   Tarsi, Luca ^a   Tedesco, Giovanna ^a   Terreni, Silvia ^a   Worby, Angela ^b   Heibreder, Christian ^c   Micheli, Fabrizio ^a  

^a GSK   (Italy)

^b GLAXOSMITHKLINE   (United Kingdom)

^c RECKITT BENCKISER   (United Kingdom)

Author keywords

Azabicyclo 3.1.0 hexanes; Dopamine D3 antagonists; hERG channel; Receptors

Indexed keywords

2 METHYL 5 [4 METHYL 5 [4 [1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEX 3 YL]BUTYL] 4H 1,2,4 TRIAZOL 3 YL]QUINOLINE; 3 [ 4 [4 METHYL 5 (2 METHYL 3 PYRIDINYL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [ 4 [4 METHYL 5 (4 PYRIDAZINYL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [ 4 [4 METHYL 5 (5 METHYL 2 PYRAZINYL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [ 4 [4 METHYL 5 (6 METHYL 3 PYRIDINYL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [ 4 [4 METHYL 5 [2 METHYL 6 (TRIFLUOROMETHYL) 3 PYRIDINYL] 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 (1 METHYL 1H PYRROL 2 YL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 (1,3,5 TRIMETHYL 1H PYRAZOL 4 YL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 (2 METHYL 1,3 THIAZOL 5 YL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 (3 THIENYL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 (4 METHYL 1,3 THIAZOL 5 YL) 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 [2 (METHYLOXY)PHENYL] 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 [3 (METHYLOXY)PHENYL] 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 [4 (METHYLOXY)PHENYL] 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [4 METHYL 5 [4 [(TRIFLUOROMETHYL)OXY]PHENYL] 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (2 CHLOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (2 FLUOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (2,4 DIFLUOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (2,4 DIMETHYL 1,3 THIAZOL 5 YL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (3 CHLOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (3 FLUOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (3,5 DIFLUOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 [5 (4 FLUOROPHENYL) 4 METHYL 4H 1,2,4 TRIAZOL 3 YL]BUTYL] 1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEXANE; 3 [4 METHYL 5 [4 [1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEX 3 YL]BUTYL] 4H 1,2,4 TRIAZOL 3 YL]BENZONITRILE; 4 [4 METHYL 5 [4 [1 [4 (TRIFLUOROMETHYL)PHENYL] 3 AZABICYCLO[3.1.0]HEX 3 YL]BUTYL] 4H 1,2,4 TRIAZOL 3 YL]BENZONITRILE; AZABICYCLO DERIVATIVE; DOPAMINE 3 RECEPTOR; DOPAMINE 3 RECEPTOR BLOCKING AGENT; POTASSIUM CHANNEL HERG; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG POTENCY; DRUG SELECTIVITY; FEMALE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; NONHUMAN; PRIORITY JOURNAL; RAT; STRUCTURE ACTIVITY RELATION;

ANIMALS; AZA COMPOUNDS; BICYCLO COMPOUNDS; BINDING SITES; COMPUTER SIMULATION; HEXANES; HUMANS; RATS; RECEPTORS, DOPAMINE D3; STRUCTURE-ACTIVITY RELATIONSHIP; TRIAZOLES;

EID: 77951690761     PISSN: 18607179     EISSN: 18607187     Source Type: Journal    
DOI: 10.1002/cmdc.201000026     Document Type: Article

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