Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines - PubMed (original) (raw)

. 2009 Feb 1;19(3):967-71.

doi: 10.1016/j.bmcl.2008.11.075. Epub 2008 Nov 24.

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

Affiliations

• PMID: 19109019
• DOI: 10.1016/j.bmcl.2008.11.075

Potent and selective adenosine A2A receptor antagonists: 1,2,4-Triazolo[1,5-c]pyrimidines

Bernard R Neustadt et al. Bioorg Med Chem Lett. 2009.

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.

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