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The therapeutic use of A 2A adenosine receptor (AR) antagonists for the treatment of neurodegenerative disorders, such as Parkinson and Alzheimer diseases, is a very promising approach. Moreover, the potential therapeutic role of A 2A AR antagonists to avoid both immunoescaping of tumor cells and tumor development is well documented. Herein, we report on the synthesis and biological evaluation of a new set of piperazine- and piperidine- containing 7-amino-2-(furan-2-yl)thiazolo[5,4- d ]pyrimidine derivatives designed as human A 2A AR antagonists/inverse agonists. Binding and potency data indicated that a good number of potent and selective hA 2A AR inverse agonists were found. Amongst them, the 2-(furan-2-yl)- N  5 -(2-(4-phenylpiperazin-1-yl)ethyl)thiazolo[5,4- d ]pyrimidine-5,7-diamine 11 exhibited the highest A 2A AR binding affinity (K i = 8.62 nM) as well as inverse agonist potency (IC 50 = 7.42 nM). In addition, bioinformatics prediction using the web tool SwissADME revealed that 8 , 11 , and 19 possessed good drug-likeness profiles.

Piperazine- and Piperidine-Containing Thiazolo[5,4-d]pyrimidine Derivatives as New Potent and Selective Adenosine A2A Receptor Inverse Agonists