Discovery of a novel class of zwitterionic, potent, selective and orally active S1P1 direct agonists

Amido-1,3,4-thiadiazoles were identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype-1 agonists. Starting from a micromolar HTS compound we developed a robust structural–activity relationship, to get to a lead that demonstrated good selectivity and ex...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 2012-12, Vol.22 (24), p.7672-7676
Hauptverfasser:	Aguilar, Nuria, Mir, Marta, Grima, Pedro M., López, Manel, Segarra, Victor, Esteban, Laia, Moreno, Imma, Godessart, Nuria, Tarrasón, Gema, Domenech, Teresa, Vilella, Dolors, Armengol, Clara, Córdoba, Mònica, Sabaté, Mar, Casals, Daniel, Domínguez, Maria
Format:	Artikel
Sprache:	eng
Schlagworte:	Administration, Oral agonists animal models Animals Biological and medical sciences chemistry Crystallography, X-Ray Disease Models, Animal Dose-Response Relationship, Drug Drug Discovery Encephalomyelitis, Autoimmune, Experimental - drug therapy Homology Lymphopenia - blood Medical sciences Models, Molecular Molecular Structure Pharmacology. Drug treatments Rats Receptors, Lysosphingolipid - agonists Sphingosine 1-phosphate Structure-Activity Relationship Thiadiazoles - administration & dosage Thiadiazoles - chemical synthesis Thiadiazoles - pharmacology zwitterions
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