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10.1021/ml100228m

http://scihub22266oqcxt.onion/10.1021/ml100228m
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C4018108!4018108 !24900287
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suck abstract from ncbi


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pmid24900287
      ACS+Med+Chem+Lett 2011 ; 2 (2 ): 102-6
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  • Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1) #MMPMID24900287
  • Lanman BA ; Cee VJ ; Cheruku SR ; Frohn M ; Golden J ; Lin J ; Lobera M ; Marantz Y ; Muller KM ; Neira SC ; Pickrell AJ ; Rivenzon-Segal D ; Schutz N ; Sharadendu A ; Yu X ; Zhang Z ; Buys J ; Fiorino M ; Gore A ; Horner M ; Itano A ; McElvain M ; Middleton S ; Schrag M ; Vargas HM ; Xu H ; Xu Y ; Zhang X ; Siu J ; Bürli RW
  • ACS Med Chem Lett 2011[Feb]; 2 (2 ): 102-6 PMID24900287 show ga
  • Optimization of a benzofuranyl S1P1 agonist lead compound (3) led to the discovery of 1-(3-fluoro-4-(5-(2-fluorobenzyl)benzo[d]thiazol-2-yl)benzyl)azetidine-3-carboxylic acid (14), a potent S1P1 agonist with minimal activity at S1P3. Dosed orally at 0.3 mg/kg, 14 significantly reduced blood lymphocyte counts 24 h postdose and attenuated a delayed type hypersensitivity (DTH) response to antigen challenge.
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