1372633-66-3Relevant articles and documents
Optimization of a potent, orally active S1P1 agonist containing a quinolinone core
Harrington, Paul E.,Croghan, Michael D.,Fotsch, Christopher,Frohn, Mike,Lanman, Brian A.,Pennington, Lewis D.,Pickrell, Alexander J.,Reed, Anthony B.,Sham, Kelvin K. C.,Tasker, Andrew,Arnett, Heather A.,Fiorino, Michael,Lee, Matthew R.,McElvain, Michele,Morrison, Henry G.,Xu, Han,Xu, Yang,Zhang, Xuxia,Wong, Min,Cee, Victor J.
, p. 74 - 78 (2012/04/10)
The optimization of a series of S1P1 agonists with limited activity against S1P3 is reported. A polar headgroup was used to improve the physicochemical and pharmacokinetic parameters of lead quinolinone 6. When dosed orally at 1 and 3 mg/kg, the azahydroxymethyl analogue 22 achieved statistically significant lowering of circulating blood lymphocytes 24 h postdose. In rats, a dose-proportional increase in exposure was measured when 22 was dosed orally at 2 and 100 mg/kg.
