Antagonists of the human adenosine A2A receptor.: Part 1:: Discovery and synthesis of thieno[3,2-d] pyrimidine-4-methanone derivatives

被引：34

作者：

Gillespie, Roger J. ^{[2
]}

Adams, David R. ^{[2
]}

Bebbington, David ^{[2
]}

Benwell, Karen ^{[2
]}

Cliffe, Ian A. ^{[2
]}

Dawson, Claire E. ^{[2
]}

Dourish, Colin T. ^{[2
]}

Fletcher, Allan ^{[2
]}

Gaur, Suneel ^{[2
]}

Giles, Paul R. ^{[2
]}

Jordan, Allan M. ^{[1
]}

Knight, Antony R. ^{[2
]}

Knutsen, Lars J. S. ^{[2
]}

Lawrence, Anthony ^{[2
]}

Lerpiniere, Joanne ^{[2
]}

Misra, Anil ^{[2
]}

Porter, Richard H. P. ^{[2
]}

Pratt, Robert M. ^{[2
]}

Shepherd, Robin ^{[2
]}

Upton, Rebecca ^{[2
]}

Ward, Simon E. ^{[2
]}

Weiss, Scott M. ^{[2
]}

Williamson, Douglas S. ^{[1
]}

机构：

[1] Vernalis R&D Ltd, Cambridge CB21 6GB, England

[2] Vernalis R&D Ltd, Winnersh RG41 5UA, Wokingham, England

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2008年 / 18卷 / 09期

关键词：

adenosine A(2A) receptor; Parkinson's disease; mefloquine;

D O I：

10.1016/j.bmcl.2008.03.075

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

The (-)-(11R,2'S)-enantiomer of the antimalarial drug mefloquine has been found to be a reasonably potent and moderately selective adenosine A(2A) receptor antagonist. Further investigation of this compound has led to the discovery of a series of keto-aryl thieno[3,2-d]pyrimidine derivatives, which are potent and selective antagonists of the adenosine A(2A) receptor. These derivatives show selectivity against the A(1) receptor. Furthermore, some of these compounds have been shown to have in vivo activity in a commonly used model, suggesting the potential for the treatment of Parkinson's disease. (C) 2008 Elsevier Ltd. All rights reserved.

引用

页码：2916 / 2919

页数：4

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