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Pyrazole derived from (+)-3-Carene; a Novel Potent and Selective Scaffold for Sphingosine-1-Phosphate (S1P1) Receptor Agonists

Zecri, Frederic and Albert, Rainer and Landrum, Gregory and Hinterding, Klaus and Cooke, Nigel Graham and Guerini, Danilo and Streiff, Markus and Bruns, Christian and Nuesslein-Hildesheim, Barbara (2009) Pyrazole derived from (+)-3-Carene; a Novel Potent and Selective Scaffold for Sphingosine-1-Phosphate (S1P1) Receptor Agonists. Bioorganic & Medicinal Chemistry Letters, 20 (1). pp. 35-37. ISSN 1464-3405

Abstract

High throughput screening and hit to lead optimization led to the identification of ‘Carene’ as a promising scaffold showing selective S1P1 receptor agonism. In parallel to this work we have establish a pharmacophore model for the S1P1 receptor highlighting the minimal structural requirement necessary for potent receptor agonism.

Item Type: Article
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Additional Information: author can archive post-print (ie final draft post-refereeing); Publisher's version/PDF cannot be used
Keywords: S1P1 Agonist; Carene; Pharmacophore
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Date Deposited: 13 Oct 2015 13:17
Last Modified: 13 Oct 2015 13:17
URI: https://oak.novartis.com/id/eprint/1459

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