ABSTRACT

AR Agonists ...............................................................................................16 2.2.1 Optimization of

N

-Substitution of Adenosine in Binding to the A

AR ...................................................................16 2.2.2 Combination of

N

-Substitution of Adenosine with 5

-Uronamide Modification to Achieve A

AR Selectivity..............22 2.2.3 Other 5

-Position Modifications.......................................................23 2.2.4 Optimization of the 2-Position of Adenosine

in Binding to the A

AR ...................................................................23 2.2.5 Optimization of the Ribose Moiety of Adenosine

in Binding to the A

AR ...................................................................25 2.2.6 Agonists for Reengineered A

ARs: Neoceptors..............................26 2.3 A

AR Antagonists ..........................................................................................26 2.3.1 Dihydropyridines and Pyridines.......................................................29 2.3.2 Flavonoids ........................................................................................30 2.3.3 Triazoloquinazolines ........................................................................30 2.3.4 Triazoloquinoxalines ........................................................................30 2.3.5 Triazolopurines .................................................................................30 2.3.6 Pyrazolotriazolopyrimidines.............................................................31 2.3.7 Pyrazoloquinolines ...........................................................................31 2.3.8 Isoquinolines and Quinazolines .......................................................31 2.3.9 Thiazoles and Thiadiazoles ..............................................................32 2.3.10 Fused Xanthines: Purinones and Purinediones................................32 2.3.11 Adenine and Adenosine Derivatives ................................................33