Johnson & Johnson Pharmaceutical Research and Development, L.L.C. , Welsh and McKean Roads, P.O. Box 776, Spring House, Pennsylvania 19477, United States.
ACS Chem Neurosci. 2011 Oct 19;2(10):555-67. doi: 10.1021/cn2000537. Epub 2011 Jun 21.
This Review summarizes and updates the work on adenosine A(2A) receptor antagonists for Parkinson's disease from 2006 to the present. There have been numerous publications, patent applications, and press releases within this time frame that highlight new medicinal chemistry approaches to this attractive and promising target to treat Parkinson's disease. The Review is broken down by scaffold type and will discuss the efforts to optimize particular scaffolds for activity, pharmacokinetics, and other drug discovery parameters. The majority of approaches focus on preparing selective A(2A) antagonists, but a few approaches to dual A(2A)/A(1) antagonists will also be highlighted. The in vivo profiles of compounds will be highlighted and discussed to compare activities across different chemical series. A clinical report and update will be given on compounds that have entered clinical trials.
这篇综述总结和更新了 2006 年至今有关腺苷 A（2A）受体拮抗剂治疗帕金森病的研究进展。在此期间，有大量出版物、专利申请和新闻稿强调了针对这一有吸引力和有前景的治疗帕金森病靶点的新型药物化学方法。综述按支架类型进行了划分，并将讨论针对特定支架的活性、药代动力学和其他药物发现参数进行优化的努力。大多数方法都集中在制备选择性 A（2A）拮抗剂上，但也将重点介绍一些双重 A（2A）/A（1）拮抗剂的方法。将突出并讨论化合物的体内概况，以比较不同化学系列的活性。将提供已进入临床试验的化合物的临床报告和更新。
