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10.1021/ml100227q

http://scihub22266oqcxt.onion/10.1021/ml100227q
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C4017978!4017978!24900286
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suck abstract from ncbi


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pmid24900286      ACS+Med+Chem+Lett 2011 ; 2 (2): 97-101
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  • Benzofuran Derivatives as Potent, Orally Active S1P1 Receptor Agonists: A Preclinical Lead Molecule for MS #MMPMID24900286
  • Saha AK; Yu X; Lin J; Lobera M; Sharadendu A; Chereku S; Schutz N; Segal D; Marantz Y; McCauley D; Middleton S; Siu J; Bürli RW; Buys J; Horner M; Salyers K; Schrag M; Vargas HM; Xu Y; McElvain M; Xu H
  • ACS Med Chem Lett 2011[Feb]; 2 (2): 97-101 PMID24900286show ga
  • 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.
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