| Literature DB >> 19109019 |
Bernard R Neustadt1, Hong Liu, Jinsong Hao, William J Greenlee, Andrew W Stamford, Carolyn Foster, Leyla Arik, Jean Lachowicz, Hongtao Zhang, Rosalia Bertorelli, Silva Fredduzzi, Geoffrey Varty, Mary Cohen-Williams, Kwokei Ng.
Abstract
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.Entities:
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Year: 2008 PMID： 19109019 DOI： 10.1016/j.bmcl.2008.11.075
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823