Synthesis, modelling and NK1 antagonist evaluation of a non-rigid cyclopropane-containing analogue of CP-99,994

被引：1
|
作者：
Aitken, DJ
Ongeri, S
Vallée-Goyet, D
Gramain, JC
Husson, HP
机构：
[1] CNRS, Lab Chim Therapeut, F-75270 Paris 06, France
[2] Univ Paris 05, Fac Sci Pharmaceut & Biol, UMR 8638, F-75270 Paris, France
[3] Univ Clermont Ferrand 2, Dept Chim, UMR 6504, CNRS,Lab SEESIB, F-63177 Aubiere, France
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2001年 / 11卷 / 05期
关键词：
D O I：
10.1016/S0960-894X(01)00020-8
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A non-rigid cyclopropane-containing diamine analogue of CP-99,994 was synthesised and was found to have only moderate NK1 receptor binding affinity. Molecular dynamics calculations of the conformational space of the former compound gave good correlation between observed activity and a recently published pharmacophore model, lending predictive value to the latter. (C) 2001 Elsevier Science Ltd. All rights reserved.
引用
收藏
页码：659 / 661
页数：3
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