Department of Chemical Research, Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033-1310, USA.
Bioorg Med Chem Lett. 2009 Feb 1;19(3):967-71. doi: 10.1016/j.bmcl.2008.11.075. Epub 2008 Nov 24.
Antagonism of the adenosine A(2a) receptor offers great promise in the treatment of Parkinson's disease. In the course of exploring pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine A(2A) antagonists, which led to clinical candidate SCH 420814, we prepared 1,2,4-triazolo[1,5-c]pyrimidines with potent and selective (vs A(1)) A(2a) antagonist activity, including oral activity in the rat haloperidol-induced catalepsy model. Structure-activity relationships and plasma levels are described for this series.
腺苷 A(2a)受体拮抗剂在治疗帕金森病方面具有巨大的潜力。在探索吡唑并[4,3-e]-1,2,4-三唑并[1,5-c]嘧啶 A(2A)拮抗剂的过程中，我们制备了具有强效和选择性（相对于 A(1)）A(2a)拮抗活性的 1,2,4-三唑并[1,5-c]嘧啶类化合物，包括在大鼠氟哌啶醇诱导的僵住模型中的口服活性。本文描述了该系列化合物的构效关系和血浆水平。
