Design and synthesis of new tricyclic indoles as potent modulators of the S1P sub(1) receptor

Modulators of S1P sub(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 sub(1) chemotypes were designed and optimized for potency and oral bioavailability. These new agent...

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Published inBioorganic & medicinal chemistry letters Vol. 25; no. 3; pp. 659 - 663
Main Authors Buzard, Daniel J, Schrader, Thomas O, Zhu, Xiuwen, Lehmann, Juerg, Johnson, Ben, Kasem, Michelle, Kim, Sun Hee, Kawasaki, Andrew, Lopez, Luis, Moody, Jeanne, Han, Sangdon, Gao, Yinghong, Edwards, Jeff, Barden, Jeremy, Thatte, Jayant, Gatlin, Joel, Jones, Robert M
Format Journal Article
LanguageEnglish
Published 01.02.2015
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Summary:Modulators of S1P sub(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 sub(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 sub(1) receptor.
Bibliography:ObjectType-Article-1
SourceType-Scholarly Journals-1
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ISSN:0960-894X
DOI:10.1016/j.bmcl.2014.11.089