کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10596642 | 981907 | 2012 | 6 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Fused tricyclic indoles as S1P1 agonists with robust efficacy in animal models of autoimmune disease
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موضوعات مرتبط
مهندسی و علوم پایه
شیمی
شیمی آلی
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چکیده انگلیسی
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.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 13, 1 July 2012, Pages 4404-4409
Journal: Bioorganic & Medicinal Chemistry Letters - Volume 22, Issue 13, 1 July 2012, Pages 4404-4409
نویسندگان
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,