Author/Authors :
Justine Y. Q. Lai، نويسنده , , Paul J. Cox، نويسنده , , Rajesh Patel، نويسنده , , Shazia Sadiq، نويسنده , , David J. Aldous، نويسنده , , Sukanthini Thurairatnam، نويسنده , , Keith Smith، نويسنده , , Darren Wheeler، نويسنده , , Savita Jagpal، نويسنده , , Sofia Parveen، نويسنده , , Gary Fenton، نويسنده , , Trevor K. P. Harrison، نويسنده , , Clive McCarthy، نويسنده , , Paul Bamborough، نويسنده ,
Abstract :
A series of oxindoles demonstrating inhibition of the phosphorylation of biotinylated substrates of Syk and IgE/Fc RI triggered basophil cell degranulation has been identified. A study of the SAR around sulfonamide 31 (IC50=5 nM, EC50=1400 nM) is discussed. The modest cellular activity representative of the sulfonamide series was overcome when the Polar Surface Area was lowered to <110 Å2, leading to the identification of amide 32 (IC50=145 nM, EC50=100 nM).
