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Biaryl and heteroaryl derivatives of SCH 58261 as potent and selective adenosine A2A receptor antagonists.

作者信息

Shah Unmesh, Boyle Craig D, Chackalamannil Samuel, Neustadt Bernard R, Lindo Neil, Greenlee William J, Foster Carolyn, Arik Leyla, Zhai Ying, Ng Kwokei, Wang Shiyong, Monopoli Angela, Lachowicz Jean E

机构信息

Schering-Plough Research Institute, 2015 Galloping Hill Road, Kenilworth, NJ 07033, USA.

出版信息

Bioorg Med Chem Lett. 2008 Jul 15;18(14):4199-203. doi: 10.1016/j.bmcl.2008.05.074. Epub 2008 May 22.

DOI:10.1016/j.bmcl.2008.05.074
PMID:18562199
Abstract

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.

摘要

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