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Pyrazole derived from (+)-3-carene; a novel potent,selective scaffold for sphingosine-1-phosphate (S1P1) receptor agonists |
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| Authors: | Frédéric J. Zécri Rainer Albert Gregory Landrum Klaus Hinterding Nigel G. Cooke Danilo Guerini Markus Streiff Christian Bruns Barbara Nuesslein-Hildesheim |
| Affiliation: | 1. Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland;2. Gerbergässlein 8/III, CH-4051 Basel, Switzerland;3. F. Hoffmann-La Roche Ltd, CH-4070 Basel, Switzerland |
| 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 established a pharmacophore model for the S1P1 receptor highlighting the minimal structural requirement necessary for potent receptor agonism. |
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