Bioorganic & Medicinal Chemistry Letters 2010-01-01

Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.

Frédéric J Zécri, Rainer Albert, Gregory Landrum, Klaus Hinterding, Nigel G Cooke, Danilo Guerini, Markus Streiff, Christian Bruns, Barbara Nuesslein-Hildesheim

Index: Bioorg. Med. Chem. Lett. 20(1) , 35-7, (2010)

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Abstract

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.Copyright 2009 Elsevier Ltd. All rights reserved.