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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Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: American Chemical Society 2010
Accesso online: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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