Structure-activity relationships of oxime neurokinin antagonists: Oxime modifications

被引：2
|
作者：
Reichard, GA [1 ]
Spitler, J [1 ]
Aslanian, R [1 ]
Mutahi, MW [1 ]
Shih, NY [1 ]
Lin, L [1 ]
Ting, PC [1 ]
Anthes, JC [1 ]
Piwinski, JJ [1 ]
机构：
[1] Schering Plough Corp, Res Inst, Kenilworth, NJ 07033 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2002年 / 12卷 / 05期
关键词：
D O I：
10.1016/S0960-894X(02)00027-6
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A thorough SAR study of the oxime region of the dual NK1/NK2 antagonist 1 revealed several modifications that result in potent dual antagonists. Follow up SAR studies on a second-generation scaffold demonstrate that certain polar groups on the oxime can improve the dual binding affinity to the subnanomolar range. (C) 2002 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：833 / 836
页数：4
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