Discovery of a Potent, S1P3-Sparing Benzothiazole Agonist of Sphingosine-1-Phosphate Receptor 1 (S1P1)
ACS Medicinal Chemistry Letters2010Vol. 2(2), pp. 102–106
Citations Over TimeTop 16% of 2010 papers
Brian A. Lanman, Victor J. Cee, Srinivasa R. Cheruku, Mike Frohn, Jennifer E. Golden, Jian Lin, Mercedes Lobera, Yael Marantz, Kristine Muller, Susana Neira, Alexander J. Pickrell, Dalia Rivenzon‐Segal, Nili Schutz, Anurag Sharadendu, Yu Xiang, Zhaoda Zhang, Janet Buys, Mike Fiorino, Anu Gore, Michelle Horner, Andrea Itano, Michele McElvain, Scot Middleton, Michael Schrag, Hugo M. Vargas, Han Xu, Yang Xu, Xuxia Zhang, Jerry Siu, Roland W. Bürli
Abstract
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.
Related Papers
- → Enhancement of Neoangiogenesis and Follicle Survival by Sphingosine-1-Phosphate in Human Ovarian Tissue Xenotransplants(2011)198 cited
- → ABCA1, ABCG1, and SR-BI: Transit of HDL-associated sphingosine-1-phosphate(2011)25 cited
- → Sphingosine 1-Phosphate Receptor 1 as a Useful Target for Treatment of Multiple Sclerosis(2012)20 cited
- Analysis of a Sphingosine 1-phosphate Receptor $hS1P_3$ in Rat Hepatoma Cells(2002)
- → The sphingosine-1-phosphate receptor agonist FTY720 promotes peripheral nerve regeneration(2014)