N-aryl cinnamides: A novel class of rigid and highly potent leukotriene B-4 receptor antagonists

被引:6
作者
Greenspan, PD
Main, AJ
Bhagwat, SS
Barsky, LI
Doti, RA
Engle, AR
Frey, LM
Zhou, HH
Lipson, KE
Chin, MH
Jackson, RH
UzielFusi, S
机构
[1] Arthr. and Bone Metabolism Research, Novartis Pharmaceuticals Corporation, Summit
关键词
D O I
10.1016/S0960-894X(97)00134-0
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
A series of N-aryl cinnamides has been prepared and assayed for antagonism of the leukotriene B-4 receptor. Several compounds in this series were found to be highly potent antagonists of the human neutrophil receptor, based on a whole cell binding assay, as well as a neutrophil aggregration assay. This series is unique among LTB4 antagonists, due to its high degree of rigidity. (C) 1997 Elsevier Science Ltd.
引用
收藏
页码:949 / 954
页数:6
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