Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

Roger J Gillespie; Ian A Cliffe; Claire E Dawson; Colin T Dourish; Suneel Gaur; Paul R Giles; Allan M Jordan; Antony R Knight; Anthony Lawrence; Joanne Lerpiniere; Anil Misra; Robert M Pratt; Richard S Todd; Rebecca Upton; Scott M Weiss; Douglas S Williamson

doi:10.1016/j.bmcl.2008.03.076

Antagonists of the human adenosine A2A receptor. Part 2: Design and synthesis of 4-arylthieno[3,2-d]pyrimidine derivatives

Bioorg Med Chem Lett. 2008 May 1;18(9):2920-3. doi: 10.1016/j.bmcl.2008.03.076. Epub 2008 Mar 30.

Authors

Roger J Gillespie¹, Ian A Cliffe, Claire E Dawson, Colin T Dourish, Suneel Gaur, Paul R Giles, Allan M Jordan, Antony R Knight, Anthony Lawrence, Joanne Lerpiniere, Anil Misra, Robert M Pratt, Richard S Todd, Rebecca Upton, Scott M Weiss, Douglas S Williamson

Affiliation

¹ Vernalis (R&D) Ltd, 613 Reading Road, Winnersh, Wokingham RG41 5UA, UK.

PMID: 18407496
DOI: 10.1016/j.bmcl.2008.03.076

Abstract

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.

MeSH terms

Adenosine A1 Receptor Antagonists
Adenosine A2 Receptor Antagonists*
Adenosine A3 Receptor Antagonists
Antiparkinson Agents / chemical synthesis
Antiparkinson Agents / therapeutic use*
Drug Design*
Humans
Models, Chemical
Parkinsonian Disorders / drug therapy*
Pyrimidines / chemical synthesis
Pyrimidines / therapeutic use*
Stereoisomerism
Structure-Activity Relationship

Substances

Adenosine A1 Receptor Antagonists
Adenosine A2 Receptor Antagonists
Adenosine A3 Receptor Antagonists
Antiparkinson Agents
Pyrimidines