Long-chain formoterol analogues:: an investigation into the effect of increasing amino-substituent chain length on the β2-adrenoceptor activity

被引:41
作者
Alikhani, V [1 ]
Beer, D [1 ]
Bentley, D [1 ]
Bruce, I [1 ]
Cuenoud, BM [1 ]
Fairhurst, RA [1 ]
Gedeck, P [1 ]
Haberthuer, S [1 ]
Hayden, C [1 ]
Janus, D [1 ]
Jordan, L [1 ]
Lewis, C [1 ]
Smithies, K [1 ]
Wissler, E [1 ]
机构
[1] Novartis Horsham Res Ctr, Horsham RH12 5AB, W Sussex, England
关键词
D O I
10.1016/j.bmcl.2004.06.086
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
The synthesis of a series of long-chain formoterol analogues in which the terminal ether residue of the beta-phenethyl-amino-substituent has been extended beyond the methyl ether residue present in the parent compound are described. Evaluation of these analogues as beta(2)-adrenoceptor agonists was used to provide an insight into the factors controlling the magnitude and duration of receptor activation. (C) 2004 Elsevier Ltd. All rights reserved.
引用
收藏
页码:4705 / 4710
页数:6
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