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Starting from a prototypical structure 1 , we describe our efforts to design and obtain novel quinazoline/pyrimidine-2,4(1 H ,3 H )-diones with high CB2 agonist potency and selectivity as well as improved physicochemical characteristics, mainly hydrophilicity. The most potent and selective CB2 agonists, 8 and 36 , in this series were also endowed with lower logP values than that of GW842166X and lead compound 1 . These derivatives appear to be promising lead compounds for the development of future CB2 agonists.

Development of Quinazoline/Pyrimidine-2,4(1H,3H)-diones as Agonists of Cannabinoid Receptor Type 2