8-Substituted 2-alkynyl-N9-propargyladenines as A2A adenosine receptor antagonists

Add time:08/14/2019    Source:sciencedirect.com

Structure–activity relationships of 2-alkynyladenine derivatives were explored by varying substituents at the 9-, 8- and 2-positions of the purine moiety in order to optimize A2A adenosine receptor antagonist activity in vitro. A propargyl group at the 9-position was found to be important for A2A antagonist activity, and the introduction of a halogen, aryl, or heteroaryl at the 8-position further enhanced activity. A series of 8-substituted 2-alkynyl-N9-propargyladenine derivatives exhibited potent antagonist activity, with IC50 values in the low nM range. Compound 4a from this series was found to be orally active at a dose of 3 mg/kg in a mouse catalepsy model and a 6-hydroxydopamine-lesioned rat model of Parkinson’s disease.

We also recommend Trading Suppliers and Manufacturers of 2-(7-Octyn-1-yl)-1H-isoindole-1,3-dione (cas 17170-26-2). Pls Click Website Link as below: cas 17170-26-2 suppliers

Prev:Fast and highly selective detection of acetaldehyde in liquor and spirits by forming aggregation-induced emission luminogen
Next:Synthesis and Myelostimulatory Activity of 1-(2-Ethoxyethyl) Piperidine Derivatives☆)