Unknown

Dataset Information

0

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.

ABSTRACT: Movement disorders such as Parkinson's disease and Huntington's disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, that is, the A(2A) AR. To further this goal, we have synthesized and characterized pharmacologically a family of high affinity A(2A) AR ligands, based on the known antagonist, SCH 442416 (R=-Me), which have structural variability on the terminus (R=-Et, -i-Pr, -allyl, and others). A O-fluoroethyl analogue suitable for use as a PET tracer had a K(i) value of 12.4 nM and was highly selective for the A(2A) AR in comparison to the A(1) and A(3) ARs.

SUBMITTER: Shinkre BA 

PROVIDER: S-EPMC2946083 | biostudies-literature | 2010 Oct

REPOSITORIES: biostudies-literature

Json Xml
altmetric image

Publications

Synthesis and evaluation of 1,2,4-triazolo[1,5-c]pyrimidine derivatives as A2A receptor-selective antagonists.

Shinkre Bidhan A BA   Kumar T Santhosh TS   Gao Zhan-Guo ZG   Deflorian Francesca F   Jacobson Kenneth A KA   Trenkle William C WC  

Bioorganic & medicinal chemistry letters 20100810 19

Movement disorders such as Parkinson's disease and Huntington's disease are serious life-limiting and debilitating movement disorders. Their onset typically occurs from mid-life to late in life, and effective diagnostic techniques for detecting and following the disease course are lacking. Our goal is to develop receptor imaging agents for positron emission tomography (PET) that selectively target the most relevant subtype of adenosine receptors (AR) that are highly expressed in the striatum, th  ...[more]

Similar Datasets

Unknown IBD-mediated oxidative cyclization of pyrimidinylhydrazones and concurrent Dimroth rearrangement: Synthesis of [1,2,4]triazolo[1,5-c]pyrimidine derivatives.
| S-EPMC3869367 | biostudies-literature
Unknown Design, synthesis and evaluation of photoactivatable derivatives of microtubule (MT)-active [1,2,4]triazolo[1,5-a]pyrimidines.
| S-EPMC5993642 | biostudies-literature
Unknown Bitopic fluorescent antagonists of the A2A adenosine receptor based on pyrazolo[4,3-e][1,2,4]triazolo[1,5-c]pyrimidin-5-amine functionalized congeners.
| S-EPMC5729930 | biostudies-literature
Unknown Bis(cyanato-?N)bis-(5,7-dimethyl-1,2,4-triazolo[1,5-a]pyrimidine-?N)zinc.
| S-EPMC3052141 | biostudies-literature
Unknown Synthesis and evaluation of 1,2,4-triazolo[1,5-a]pyrimidines as antibacterial agents against Enterococcus faecium.
| S-EPMC4633020 | biostudies-literature
Unknown 2-Phenyl-8,9,10,11-tetra-hydro-1-benzo-thieno[3,2-e][1,2,4]triazolo[1,5-c]pyrimidine.
| S-EPMC3099952 | biostudies-literature
Unknown Synthesis and biological evaluation of a new series of 1,2,4-triazolo[1,5-a]-1,3,5-triazines as human A(2A) adenosine receptor antagonists with improved water solubility.
| S-EPMC3578427 | biostudies-literature
Unknown Crystal structure and Hirshfeld surface analysis of 5-methyl-1,2,4-triazolo[1,5-a]pyrimidine.
| S-EPMC6281126 | biostudies-other
Unknown 1,2,4-Triazolo[1,5-a]pyrimidines in drug design.
| S-EPMC6394845 | biostudies-literature
Unknown Synthesis and characterization of 1,2,4-triazolo[1,5-a]pyrimidine-2-carboxamide-based compounds targeting the PA-PB1 interface of influenza A virus polymerase.
| S-EPMC7561591 | biostudies-literature