Structure-activity relationships of 2-amino-3-aroyl-4-[(4-arylpiperazin-1- yl)methyl]thiophenes. Part 2: Probing the influence of diverse substituents at the phenyl of the arylpiperazine moiety on allosteric enhancer activity at the A 1 adenosine receptor

Bioorganic and Medicinal Chemistry

Volumn 20, Issue 2, 2012, Pages 996-1007

  Romagnoli, Romeo ^a   Baraldi, Pier Giovanni ^a   Carrion, Maria Dora ^a   Cara, Carlota Lopez ^a   Cruz Lopez, Olga ^a   Salvador, Maria Kimatrai ^a   Preti, Delia ^a   Tabrizi, Mojgan Aghazadeh ^a   Shryock, John C ^b   Moorman, Allan R ^c   Vincenzi, Fabrizio ^a   Varani, Katia ^a   Borea, Pier Andrea ^a  

^a UNIVERSITY OF FERRARA   (Italy)

^b UNIVERSITY OF FLORIDA COLLEGE OF MEDICINE   (United States)

^c King Pharmaceuticals Inc   (United States)

Author keywords

2 Amino 3 benzoylthiophene; A 1 adenosine receptor; Allosteric enhancer; G protein coupled receptors

Indexed keywords

1 [4 [5 AMINO 4 (4 CHLOROBENZOYL)THIOPHEN 3 YLMETHYL]PIPERAZIN 1 YL] 2 (4 CHLOROPHENYL)ETHANONE; 2 [4 [5 AMINO 4 (4 CHLOROBENZOYL)THIOPHEN 3 YLMETHYL]PIPERAZIN 1 YL] 2 (4 CHLOROPHENYL)ETHANONE; 2 AMINO 3 AROYL 4 [(4 ARYLPIPERAZIN 1 YL)METHYL]THIOPHENE DERIVATIVE; [2 AMINO 4 [[4 (2 CHLOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2 FLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,3 DIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,4 DIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,4,6 TRIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,5 DICHLOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,5 DIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,6 DICHLOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (2,6 DIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (3 CHLOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (3 FLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (3,4 DIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (3,5 DIFLUOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (4 CHLOROBENZOYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (4 CHLOROBENZYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (4 CHLOROPHENYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (4 FLUOROBENZYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (CYCLOPENTYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (ISOPROPYL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 (NAPHTHALEN 1 YL)PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 [2 (4 CHLOROPHENYL)ETHYL]PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; [2 AMINO 4 [[4 [2 (4 CHLOROPHENYL)PROPYL]PIPERAZIN 1 YL]METHYL]THIOPHEN 3 YL] (4 CHLOROPHENYL)METHANONE; ADENOSINE A1 RECEPTOR; ADENOSINE A1 RECEPTOR ANTAGONIST; CYCLIC AMP; PIPERAZINE DERIVATIVE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL CELL; ARTICLE; CHO CELL; CONTROLLED STUDY; DRUG MECHANISM; DRUG RECEPTOR BINDING; DRUG STRUCTURE; DRUG SYNTHESIS; DRUG TARGETING; MOLECULAR PROBE; NONHUMAN; STRUCTURE ACTIVITY RELATION; STRUCTURE ANALYSIS;

ADENOSINE A1 RECEPTOR ANTAGONISTS; ALLOSTERIC REGULATION; ANIMALS; CHO CELLS; CRICETINAE; CRICETULUS; CYCLIC AMP; HUMANS; PIPERAZINES; PROTEIN BINDING; RECEPTOR, ADENOSINE A1; STRUCTURE-ACTIVITY RELATIONSHIP; THIOPHENES;

EID: 84855775584     PISSN: 09680896     EISSN: 14643391     Source Type: Journal    
DOI: 10.1016/j.bmc.2011.11.044     Document Type: Article

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