8-Substituted-9-deazaxanthines as adenosine receptor ligands: Design, synthesis and structure-affinity relationships at A 2B

European Journal of Medicinal Chemistry

Volumn 39, Issue 10, 2004, Pages 879-887

  Carotti, Angelo ^a   Stefanachi, Angela ^a   Raviña, Enrique ^b   Sotelo, Eddy ^b   Loza, Maria Isabel ^b   Cadavid, Maria Isabel ^b   Centeno, Nuria B ^c   Nicolotti, Orazio ^a  

^a UNIVERSITY OF BARI   (Italy)

^b UNIVERSITY OF SANTIAGO DE COMPOSTELA   (Spain)

^c C/Dr Aiguader 80 08003 B   (Spain)

Author keywords

1,3 Dialkyl 6 substituted 1H pyrrolo 3,2 d pyrimidine 2,4(3H, 5H) diones; A 2A A 2B selectivity; A 2B and A 2A binding affinities; Adenosine receptor antagonists; Quantitative structure affinity relationships

Indexed keywords

1,3 DIMETHYL 5 NITRO 6 [2 (5 BROMOTHIEN 2 YL)VINYL]PYRIMIDINE 2,4(1H,3H) DIONE; 1,3 DIMETHYL 5 NITRO 6 [2 (THIEN 2 YL)VINYL]PYRIMIDINE 2,4(1H,3H) DIONE; 1,3 DIMETHYL 5 NITRO 6 [2 (THIEN 3 YL)VINYL]PYRIMIDINE 2,4(1H,3H) DIONE; 1,3 DIMETHYL 6 (5 BROMOTHIEN 2 YL) 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 1,3 DIMETHYL 6 (THIEN 3 YL) 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 1,3,5 TRIMETHYL 6 (FUR 2 YL) 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 1,3,5 TRIMETHYL 6 (THIEN 2 YL) 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 1,3,5 TRIMETHYL 6 PHENYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (2 FLUOROPHENYL) 1,3 DIMETHYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (2,6 DIFLUOROPHENYL) 1,3 DIMETHYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (4 AMINOPHENYL) 1,3 DIMETHYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (4 AMINOPHENYL) 1,3 DIPROPYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (4 BENZYLOXYPHENYL) 1,3 DIPROPYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (4 HYDROXYPHENYL) 1,3 DIMETHYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (4 PROPOXYPHENYL) 1,3 DIPROPYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 (FUR 2 YL) 1,3 DIMETHYL 1H PYRROLO[3,2 D]PYRIMIDINE 2,4(3H,5H) DIONE; 6 [2 (2 FLUOROPHENYL)VINYL] 1,3 DIMETHYL 5 NITROPYRIMIDINE 2,4(1H,3H) DIONE; 6 [2 (2,6 DIFLUOROPHENYL)VINYL] 1,3 DIMETHYL 5 NITROPYRIMIDINE 2,4(1H,3H) DIONE; 6 [2 (4 BENZYLOXYPHENYL)VINYL] 1,3 DIPROPYL 5 NITROPYRIMIDINE 2,4(1H,3H) DIONE; 6 [2 (4 HYDROXYPHENYL)VINYL] 1,3 DIMETHYL 5 NITROPYRIMIDINE 2,4(1H,3H) DIONE; 6 [2 (4 PROPOXYPHENYL)VINYL] 1,3 DIPROPYL 5 NITROPYRIMIDINE 2,4(1H,3H) DIONE; 6 [2 (FUR 2 YL)VINYL] 1,3 DIMETHYL 5 NITROPYRIMIDINE 2,4(1H,3H) DIONE; ADENOSINE A2A RECEPTOR; ADENOSINE A2B RECEPTOR; ADENOSINE A3 RECEPTOR AGONIST; ADENOSINE RECEPTOR BLOCKING AGENT; N [4 (1,3 DIMETHYL 2,4 DIOXO 2,3,4,5 TETRAHYDRO 1H PYRROLO[3,2 D]PYRIMIDIN 6 YL)PHENYL]ACETAMIDE; N [4 [2 (1,3 DIMETHYL 5 NITRO 2,6 DIOXO 1,2,3,6 TETRAHYDROPYRIMIDIN 4 YL)VINYL]PHENYL]ACETAMIDE; UNCLASSIFIED DRUG;

ARTICLE; BINDING AFFINITY; DRUG ACTIVITY; DRUG RECEPTOR BINDING; DRUG SCREENING; DRUG SYNTHESIS; PHYSICAL CHEMISTRY; QUANTITATIVE ANALYSIS; STRUCTURE ACTIVITY RELATION;

ANIMALS; CELL LINE; CHO CELLS; CRICETINAE; HUMANS; LIGANDS; PROTEIN BINDING; RECEPTOR, ADENOSINE A2B; STRUCTURE-ACTIVITY RELATIONSHIP; XANTHINES;

EID: 4644258659     PISSN: 02235234     EISSN: None     Source Type: Journal    
DOI: 10.1016/j.ejmech.2004.07.008     Document Type: Article

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