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Discovery of a Potent, S1P(3)-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P(1))

[Image: see text] Optimization of a benzofuranyl S1P(1) 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 S1P(1) agonist with minimal activity at S1P(3). Dosed orally at 0.3 mg/kg, 14 significantl...

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Detalhes bibliográficos
Main Authors: Lanman, Brian A., Cee, Victor J., Cheruku, Srinivasa R., Frohn, Mike, Golden, Jennifer, Lin, Jian, Lobera, Mercedes, Marantz, Yael, Muller, Kristine M., Neira, Susana C., Pickrell, Alexander J., Rivenzon-Segal, Dalia, Schutz, Nili, Sharadendu, Anurag, Yu, Xiang, Zhang, Zhaoda, Buys, Janet, Fiorino, Mike, Gore, Anu, Horner, Michelle, Itano, Andrea, McElvain, Michele, Middleton, Scot, Schrag, Michael, Vargas, Hugo M., Xu, Han, Xu, Yang, Zhang, Xuxia, Siu, Jerry, Bürli, Roland W.
Formato: Artigo
Idioma:Inglês
Publicado em: American Chemical Society 2010
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC4018108/
https://ncbi.nlm.nih.gov/pubmed/24900287
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/ml100228m
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