Pyrazole derived from (+)-3-Carene; a Novel Potent and Selective Scaffold for Sphingosine-1-Phosphate (S1P1) Receptor Agonists
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Zecri, Frederic, Albert, Rainer, Landrum, Gregory, Hinterding, Klaus, Cooke, Nigel Graham, Guerini, Danilo, Streiff, Markus, 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 |