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Deprecated: Implicit conversion from float 263.2 to int loses precision in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 534 ACS+Med+Chem+Lett 2011 ; 2 (2): 102-6 Nephropedia Template TP
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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 S; 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 PMID24900287show 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-carboxyl ic 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.