期刊
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
卷 18, 期 14, 页码 4199-4203出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2008.05.074
关键词
adenosine; A(2A); A(2A) receptor; A(2A) antagonist; A(2A) receptor antagonist; SCH 58261; Parkinson's Disease
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. (C) 2008 Elsevier Ltd. All rights reserved.
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