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Pyrazole derived from (+)-3-carene; a novel potent, selective scaffold for sphingosine-1-phosphate (S1P(1)) receptor agonists.
Zécri, Frédéric J; Albert, Rainer; Landrum, Gregory; Hinterding, Klaus; Cooke, Nigel G; Guerini, Danilo; Streiff, Markus; Bruns, Christian; Nuesslein-Hildesheim, Barbara.
Afiliação
  • Zécri FJ; Novartis Institutes for BioMedical Research, Novartis Campus, CH-4056 Basel, Switzerland. frederic.zecri@novartis.com
Bioorg Med Chem Lett ; 20(1): 35-7, 2010 Jan 01.
Article em En | MEDLINE | ID: mdl-19954976
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.
Assuntos

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirazóis / Monoterpenos / Receptores de Lisoesfingolipídeo Idioma: En Ano de publicação: 2010 Tipo de documento: Article

Texto completo: 1 Base de dados: MEDLINE Assunto principal: Pirazóis / Monoterpenos / Receptores de Lisoesfingolipídeo Idioma: En Ano de publicação: 2010 Tipo de documento: Article