Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P1) receptor agonists

被引：8
|
作者：
Zecri, Frederic J. [1 ]
Albert, Rainer
Landrum, Gregory [1 ]
Hinterding, Klaus [2 ]
Cooke, Nigel G. [1 ]
Guerini, Danilo [1 ]
Streiff, Markus [1 ]
Bruns, Christian [1 ]
Nuesslein-Hildesheim, Barbara [1 ]
机构：
[1] Novartis Inst BioMed Res, CH-4056 Basel, Switzerland
[2] F Hoffmann La Roche Ltd, CH-4070 Basel, Switzerland
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2010年 / 20卷 / 01期
关键词：
S1P(1) agonist; Carene; Pharmacophore model; LIGAND-BINDING POCKET; SPHINGOSINE; 1-PHOSPHATE; 3-ARYLPROPIONIC ACIDS; LYMPHOCYTE EGRESS; IDENTIFICATION; MODULATORS; DISCOVERY; AFFINITY; SUBTYPES; FTY720;
D O I：
10.1016/j.bmcl.2009.11.045
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
High throughput screening and hit to lead optimization led to the identification of 'carene' as a promising scaffold showing selective S1P(1) receptor agonism. In parallel to this work we have established a pharmacophore model for the S1P(1) receptor highlighting the minimal structural requirement necessary for potent receptor agonism. (C) 2009 Elsevier Ltd. All rights reserved.
引用
收藏
页码：35 / 37
页数：3
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