1257093-72-3Relevant academic research and scientific papers
Novel 5- and 6-subtituted benzothiazoles with improved physicochemical properties: Potent S1P1 agonists with in vivo lymphocyte-depleting activity
Frohn, Mike,Cee, Victor J.,Lanman, Brian A.,Pickrell, Alexander J.,Golden, Jennifer,Rivenzon-Segal, Dalia,Middleton, Scot,Fiorino, Mike,Xu, Han,Schrag, Michael,Xu, Yang,McElvain, Michele,Muller, Kristine,Siu, Jerry,Bürli, Roland
, p. 628 - 633 (2012)
An SAR campaign designed to increase polarity in the 'tail' region of benzothiazole 1 resulted in two series of structurally novel 5-and 6-substituted S1P1 agonists. Structural optimization for potency ultimately delivered carboxamide (+)-11f,
Discovery of a potent, S1P3-sparing benzothiazole agonist of sphingosine-1-phosphate receptor 1 (S1P1)
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,Burli, Roland W.
scheme or table, p. 102 - 106 (2011/04/12)
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 S1P
