Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
10596642 | Bioorganic & Medicinal Chemistry Letters | 2012 | 6 Pages |
Abstract
Two series of fused tricyclic indoles were identified as potent and selective S1P1 agonists. In vivo these agonists produced a significant reduction in circulating lymphocytes which translated into robust efficacy in several rodent models of autoimmune disease. Importantly, these agonists were devoid of any activity at the S1P3 receptor in vitro, and correspondingly did not produce S1P3 mediated bradycardia in telemeterized rat.
Keywords
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Daniel J. Buzard, Sangdon Han, Luis Lopez, Andrew Kawasaki, Jeanne Moody, Lars Thoresen, Brett Ullman, Juerg Lehmann, Imelda Calderon, Xiuwen Zhu, Tawfik Gharbaoui, Dipanjan Sengupta, Ashwin Krishnan, Yinghong Gao, Jeff Edwards, Jeremy Barden,