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.jpg): Failed to open stream: No such file or directory in C:\Inetpub\vhosts\kidney.de\httpdocs\pget.php on line 117 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.