4.5 Article

Design and synthesis of new tricyclic indoles as potent modulators of the S1P1 receptor

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 25, Issue 3, Pages 659-663

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2014.11.089

Keywords

S1P(1); Sphingosine-1-phosphate; Gilenya (R)

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Modulators of S1P(1) have proven utility for the treatment of autoimmune disease and efforts to identify new agents with improved safety and pharmacokinetic parameters are ongoing. Several new S1P(1) chemotypes were designed and optimized for potency and oral bioavailability. These new agents are characterized by a 'tricyclic fused indole array' and are highly potent agonists of the S1P(1) receptor. (C) 2014 Elsevier Ltd. All rights reserved.

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