Synthesis and structure-activity relationship of novel benzoxazole derivatives as melatonin receptor agonists

被引：88
|
作者：
Sun, LQ [1 ]
Chen, J [1 ]
Bruce, M [1 ]
Deskus, JA [1 ]
Epperson, JR [1 ]
Takaki, K [1 ]
Johnson, G [1 ]
Iben, L [1 ]
Mahle, CD [1 ]
Ryan, E [1 ]
Xu, C [1 ]
机构：
[1] Bristol Myers Squib, Pharmaceut Res Inst, Wallingford, CT 06492 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2004年 / 14卷 / 14期
关键词：
melatonin; melatonin receptors; agonists; benzoxazole;
D O I：
10.1016/j.bmcl.2004.04.082
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of benzoxazole derivatives was synthesized and evaluated as melatoninergic ligands. The binding affinity of these compounds for human MT1 and MT2 receptors was determined using 2-[I-125]-iodomelatonin as the radioligand. From this series of benzoxazole derivatives, compounds 14 and 17 were identified as melatonin receptor agonists. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码：3799 / 3802
页数：4
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