Biaryl and Heteroaryl Derivatives of Sch 58261 As Potent and Selective Adenosine A(2a) Receptor Antagonists
Bioorganic & medicinal chemistry letters(2008)
摘要
SCH 58261 is a reported adenosine A(2A) receptor antagonist, which is active in rat in vivo models of Parkinson's Disease upon ip administration. However, it has poor selectivity versus the A(1) receptor and does not demonstrate oral activity. We report the design and synthesis of biaryl and heteroaryl analogs of SCH 58261 which improve the A(2A) receptor binding selectivity as well as the pharmacokinetic properties of SCH 58261. In particular, the quinoline 25 has excellent A(2A) receptor in vitro binding affinity and selectivity, sustained rat plasma levels upon oral dosing, and is active orally in a rat behavioral assay.
更多查看译文
关键词
adenosine,A(2A),A(2A) receptor,A(2A) antagonist,A(2A) receptor antagonist,SCH 58261,Parkinson's Disease
AI 理解论文
溯源树
样例
生成溯源树,研究论文发展脉络
Chat Paper
正在生成论文摘要