| Literature DB >> 22633692 |
Daniel J Buzard1, 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, Michael Morgan, Khawja Usmani, Chuan Chen, Abu Sadeque, Jayant Thatte, Michelle Solomon, Lixia Fu, Kevin Whelan, Ling Liu, Hussien Al-Shamma, Joel Gatlin, Minh Le, Charles Xing, Sheryll Espinola, Robert M Jones.
Abstract
Two series of fused tricyclic indoles were identified as potent and selective S1P(1) 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 S1P(3) receptor in vitro, and correspondingly did not produce S1P(3) mediated bradycardia in telemeterized rat.Entities:
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Year: 2012 PMID： 22633692 DOI： 10.1016/j.bmcl.2012.04.129
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823