Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives.
Gillespie RJ., Cliffe IA., Dawson CE., Dourish CT., Gaur S., Giles PR., Jordan AM., Knight AR., Lawrence A., Lerpiniere J., Misra A., Pratt RM., Todd RS., Upton R., Weiss SM., Williamson DS.
We describe herein the discovery and development of a series of 4-arylthieno[3,2-d]pyrimidines which are potent adenosine A(2A) receptor antagonists. These novel compounds show high degrees of selectivity against the human A(1), A(2B) and A(3) receptor sub-types. Moreover, a number of these compounds show promising activity in vivo, suggesting potential utility in the treatment of Parkinson's disease.