Optimization of 6-heterocyclic-2-(1 H -pyrazol-1-yl)- N -(pyridin-2-yl)pyrimidin-4-Amine as potent adenosine A2A receptor antagonists for the treatment of Parkinsons disease

ACS Chemical Neuroscience

Volumn 5, Issue 8, 2014, Pages 674-682

  Zheng, Jiyue ^a   Yang, Zhaohui ^a   Li, Xuan ^a   Li, Linlang ^a   Ma, Haikuo ^a   Wang, Meiyu ^a   Zhang, Hongjian ^a   Zhen, Xuechu ^a   Zhang, Xiaohu ^a  

^a SOOCHOW UNIVERSITY   (China)

Author keywords

Adenosine receptor; antagonist; GPCR; lead optimization; Parkinsons disease

Indexed keywords

6 (2(METHOXYMETHYL)PYRROLIDIN 1 YL) 2 (1H PYRAZOL 1 YL) N (PYRIDIN 2 YL)PYRIMDINEI4 AMINE; 6 HETEROCYCLIC 2 (1H PYRAZOL 1 YL) N (PYRIDIN 2 YL)PYRIMIDIN 4 AMINE; ADENOSINE A2A RECEPTOR; ADENOSINE A2A RECEPTOR ANTAGONIST; CYCLIC AMP; CYTOCHROME P450 1A2; CYTOCHROME P450 2C19; CYTOCHROME P450 2C9; CYTOCHROME P450 2D6; CYTOCHROME P450 3A4; G PROTEIN COUPLED RECEPTOR; HETEROCYCLIC AMINE; ISTRADEFYLLINE; PRELADENANT; PYRIMIDINE DERIVATIVE; RADIOLIGAND; TOZADENANT; UNCLASSIFIED DRUG; VIPADENANT; ADENOSINE A2 RECEPTOR ANTAGONIST; ADRA2A PROTEIN, HUMAN; ALPHA 2 ADRENERGIC RECEPTOR; ANTIPARKINSON AGENT; HALOPERIDOL;

ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; BLOOD BRAIN BARRIER; CARBON NUCLEAR MAGNETIC RESONANCE; CHEMICAL STRUCTURE; CONTROLLED STUDY; DOPAMINERGIC SYSTEM; DRUG EFFICACY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG SAFETY; DRUG SYNTHESIS; ENZYME INHIBITION; HALOPERIDOL-INDUCED CATALEPSY; HEK293 CELL LINE; HUMAN; HUMAN CELL; HUMAN TISSUE; LIGAND BINDING; LIQUID CHROMATOGRAPHY; LIVER MICROSOME; MASS SPECTROMETRY; MOUSE; NEUROPHARMACOLOGY; NONHUMAN; PARKINSON DISEASE; PARKINSON DS; PRIORITY JOURNAL; PROTON NUCLEAR MAGNETIC RESONANCE; STRUCTURE ACTIVITY RELATION; ANIMAL; BRAIN; CATALEPSY; DOSE RESPONSE; DRUG EFFECTS; DRUG INTERACTION; MALE; METABOLISM; PARKINSONIAN DISORDERS; SYNTHESIS; WISTAR RAT;

ADENOSINE A2 RECEPTOR ANTAGONISTS; ANIMALS; ANTIPARKINSON AGENTS; BRAIN; CATALEPSY; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG INTERACTIONS; HALOPERIDOL; HEK293 CELLS; HUMANS; MALE; MICE; MICROSOMES, LIVER; MOLECULAR STRUCTURE; PARKINSONIAN DISORDERS; PYRIMIDINES; RATS, WISTAR; RECEPTORS, ADRENERGIC, ALPHA-2;

EID: 84906274979     PISSN: None     EISSN: 19487193     Source Type: Journal    
DOI: 10.1021/cn5000716     Document Type: Article

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