Structure-activity relationship of biaryl acylsulfonamide analogues on the human EP3 prostanoid receptor

被引:38
作者
Gallant, M [1 ]
Carrière, MC [1 ]
Chateauneuf, A [1 ]
Denis, D [1 ]
Gareau, Y [1 ]
Godbout, C [1 ]
Greig, G [1 ]
Juteau, H [1 ]
Lachance, N [1 ]
Lacombe, P [1 ]
Lamontagne, S [1 ]
Metters, KM [1 ]
Rochette, C [1 ]
Ruel, R [1 ]
Slipetz, D [1 ]
Sawyer, N [1 ]
Tremblay, N [1 ]
Labelle, M [1 ]
机构
[1] Merck Frosst Ctr Therapeut Res, Pointe Claire, PQ H9R 4P8, Canada
关键词
D O I
10.1016/S0960-894X(02)00518-8
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Potent and selective ligands for the human EP3 prostanoid receptor are described. Biaryl compounds hearing a tethered ortho substituted acidic moiety were identified as potent EP3 antagonists based on the SAR described herein. The binding affinity of key compounds on all eight human prostanoid receptors is reported. (C) 2002 Elsevier Science Ltd. All rights reserved.
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收藏
页码:2583 / 2586
页数:4
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