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Synthesis of N-pyrimidinyl-2-phenoxyacetamides as adenosine A2A receptor antagonists.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Mar 15; Vol. 18 (6), pp. 1778-83. Date of Electronic Publication: 2008 Feb 16. - Publication Year :
- 2008
-
Abstract
- A series of N-pyrimidinyl-2-phenoxyacetamide adenosine A(2A) antagonists is described. SAR studies led to compound 14 with excellent potency (K(i) = 0.4 nM), selectivity (A(1)/A(2A) > 100), and efficacy (MED 10 mg/kg p.o.) in the rat haloperidol-induced catalepsy model for Parkinson's disease.
- Subjects :
- Administration, Oral
Animals
Antiparkinson Agents pharmacology
Catalepsy chemically induced
Cytochrome P-450 CYP2D6 metabolism
Cytochrome P-450 CYP2D6 Inhibitors
Cytochrome P-450 CYP3A
Cytochrome P-450 Enzyme Inhibitors
Cytochrome P-450 Enzyme System metabolism
Electrophysiology
Ether-A-Go-Go Potassium Channels antagonists & inhibitors
Haloperidol toxicity
Humans
Molecular Structure
Phenoxyacetates chemistry
Phenoxyacetates pharmacology
Pyrimidines chemistry
Pyrimidines pharmacology
Rats
Structure-Activity Relationship
Adenosine A2 Receptor Antagonists
Antiparkinson Agents chemical synthesis
Catalepsy prevention & control
Parkinson Disease physiopathology
Phenoxyacetates chemical synthesis
Pyrimidines chemical synthesis
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 18
- Issue :
- 6
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 18329269
- Full Text :
- https://doi.org/10.1016/j.bmcl.2008.02.032