Benzofuran Derivatives as Potent, Orally Active S1P(1) Receptor Agonists: A Preclinical Lead Molecule for MS

[Image: see text] We have discovered novel benzofuran-based S1P(1) 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 S1P(1) agonist with >1000× selectivity over S1P(3). It demonstrated a go...

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Hauptverfasser: Saha, Ashis K., Yu, Xiang, Lin, Jian, Lobera, Mercedes, Sharadendu, Anurag, Chereku, Srinivas, Schutz, Nili, Segal, Dalia, Marantz, Yael, McCauley, Dilara, Middleton, Scot, Siu, Jerry, Bürli, Roland W., Buys, Janet, Horner, Michelle, Salyers, Kevin, Schrag, Michael, Vargas, Hugo M., Xu, Yang, McElvain, Michele, Xu, Han
Format: Artigo
Sprache:Inglês
Veröffentlicht: American Chemical Society 2010
Online Zugang:https://ncbi.nlm.nih.gov/pmc/articles/PMC4017978/
https://ncbi.nlm.nih.gov/pubmed/24900286
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml100227q
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