| Autor: |
Hugo M. Vargas, Yang Xu, Jerry Siu, Janet Buys, Michelle Horner, Jian Lin, Ashis Saha, Han Xu, Michele McElvain, Anurag Sharadendu, Scot Middleton, Roland Burli, Yael Marantz, Dalia Segal, Kevin Salyers, Mercedes Lobera, Dilara Mccauley, Srinivas Chereku, Xiang Yu, Nili Schutz, Michael Schrag |
| Rok vydání: |
2010 |
| Předmět: |
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| Zdroj: |
ACS Medicinal Chemistry Letters. 2:97-101 |
| ISSN: |
1948-5875 |
| Popis: |
We have discovered novel benzofuran-based S1P1 agonists with excellent in vitro potency and selectivity. 1-((4-(5-Benzylbenzofuran-2-yl)-3-fluorophenyl)methyl) azetidine-3-carboxylic acid (18) is a potent S1P1 agonist with >1000× selectivity over S1P3. It demonstrated a good in vitro ADME profile and excellent oral bioavailability across species. Dosed orally at 0.3 mg/kg, 18 significantly reduced blood lymphocyte counts 24 h postdose and demonstrated efficacy in a mouse EAE model of relapsing MS. |
| Databáze: |
OpenAIRE |
| Externí odkaz: |
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