Literature DB >> 23141913

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

Nuria Aguilar1, Marta Mir, Pedro M Grima, Manel López, Victor Segarra, Laia Esteban, Imma Moreno, Nuria Godessart, Gema Tarrasón, Teresa Domenech, Dolors Vilella, Clara Armengol, Mònica Córdoba, Mar Sabaté, Daniel Casals, Maria Domínguez.   

Abstract

Amido-1,3,4-thiadiazoles have been identified as a novel structural class of potent and selective sphingosine-1-phosphate receptor subtype 1 agonists. Starting from a micromolar HTS hit with the help of an in-house homology model, robust structural-activity relationships were developed to yield compounds with good selectivity and excellent in vivo efficacy in rat models.
Copyright © 2012 Elsevier Ltd. All rights reserved.

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Year:  2012        PMID: 23141913     DOI: 10.1016/j.bmcl.2012.09.110

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  1 in total

Review 1.  Modulators of the Sphingosine 1-phosphate receptor 1.

Authors:  Mariangela Urbano; Miguel Guerrero; Hugh Rosen; Edward Roberts
Journal:  Bioorg Med Chem Lett       Date:  2013-09-29       Impact factor: 2.823

  1 in total

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