2-Amino-N-pyrimidin-4-ylacetamides as A2A receptor antagonists: 1. Structure-activity relationships and optimization of heterocyclic substituents

Journal of Medicinal Chemistry

Volumn 51, Issue 6, 2008, Pages 1719-1729

  Slee, Deborah H ^a   Chen, Yongsheng ^a   Zhang, Xiaohu ^a   Moorjani, Manisha ^a   Lanier, Marion C ^a   Lin, Emily ^a   Rueter, Jaimie K ^a   Williams, John P ^a   Lechner, Sandra M ^b   Markison, Stacy ^b   Malany, Siobhan ^a   Santos, Mark ^a   Gross, Raymond S ^a   Jalali, Kayvon ^a   Sai, Yang ^a   Zuo, Zhiyang ^a   Yang, Chun ^a   Castro Palomino, Julio C ^c   Crespo, María I ^c   Prat, Maria ^c   Gual, Silvia ^c   Díaz, José Luis ^c   Saunders, John ^a   more..

^a Neurocrine Biosciences ^*  (United States)

^b NEUROCRINE BIOSCIENCES INC   (United States)

^c NONE   (Spain)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4 METHYLPIPERAZIN 1 YL) N (6 PYRAZOL 1 YL 2 PYRIDIN 2 YLPYRIMIDIN 4 YL)ACETAMIDE; 2 (4 METHYLPIPERAZIN 1 YL) N (6 PYRAZOL 1 YL 2 THIAZOL 2 YLPYRIMIDIN 4 YL)ACETAMIDE; 2 AMINO N PYRIMIDIN 4 YLACETAMIDE DERIVATIVE; 4 [2 [7 AMINO 2 (2 FURYL) 1,2,4 TRIAZOLO[2,3 A][1,3,5]TRIAZIN 5 YLAMINO]ETHYL]PHENOL; ADENOSINE A2A RECEPTOR ANTAGONIST; N (2 FURAN 2 YL 6 THIAZOL 2 YLPYRIMIDIN 4 YL) 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N (2,6 DIPYRAZOL 1 YLPYRIMIDIN 4 YL) 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (3,5 DIMETHYLPYRAZOL 1 YL) 6 (4 METHYLOXAZOL 5 YL)PYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (3,5 DIMETHYLPYRAZOL 1 YL) 6 OXAZOL 5 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (3,5 DIMETHYLPYRAZOL 1 YL) 6 THIAZOL 2 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (5 METHYLFURAN 2 YL) 6 (5 METHYLPYRAZOL 1 YL)PYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (5 METHYLFURAN 2 YL) 6 PYRAZOL 1 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (5 METHYLFURAN 2 YL) 6 THIAZOL 2 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [2 (THIOPEN 2 YL) 6 PYRIDIN 2 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [6 (3,5 DIMETHYLPYRAZOL 1 YL) 2 (5 METHYLFURAN 2 YL)PYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [6 (3,5 DIMETHYLPYRAZOL 1 YL) 2 FURAN 2 YL 6 THIAZOL 2 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [6 (3,5 DIMETHYLPYRAZOL 1 YL) 2 PYRIDIN 2 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; N [6 (3,5 DIMETHYLPYRAZOL 1 YL) 2 THIAZOL 2 YLPYRIMIDIN 4 YL] 2 (4 METHYLPIPERAZIN 1 YL)ACETAMIDE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CONTROLLED STUDY; DRUG MECHANISM; DRUG METABOLISM; DRUG POTENCY; DRUG STRUCTURE; DRUG SYNTHESIS; HUMAN; HUMAN CELL; LIQUID CHROMATOGRAPHY; LIVER MICROSOME; MALE; MASS SPECTROMETRY; NONHUMAN; RAT; RISK ASSESSMENT; STRUCTURE ACTIVITY RELATION;

ACETAMIDES; ANIMALS; BINDING SITES; CYCLIZATION; DRUG EVALUATION, PRECLINICAL; HEPATOCYTES; HUMANS; MICROSOMES, LIVER; MOLECULAR STRUCTURE; PYRIMIDINES; RATS; RECEPTOR, ADENOSINE A2A; STEREOISOMERISM; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 41149100118     PISSN: 00222623     EISSN: None     Source Type: Journal    
DOI: 10.1021/jm701185v     Document Type: Article

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