Author/Authors :
Yong Gong، نويسنده , , J. Kent Barbay، نويسنده , , Mieke Buntinx، نويسنده , , Jian Li، نويسنده , , Jean Van Wauwe، نويسنده , , Concha Claes، نويسنده , , Guy Van Lommen، نويسنده , , Pamela J. Hornby، نويسنده , , Wei He، نويسنده ,
Abstract :
A series of aniline-substituted tetrahydroquinoline C5a receptor antagonists were discovered. A functionality requirement of ortho substitution on the aniline was revealed. Secondary anilines, in general, outperformed tertiary analogs in inhibition of C5a-induced calcium mobilization. Further enhancement of activity was realized in the presence of an ortho hydroxyalkyl side chain. The functional IC50 of selected analogs was optimized to the single-digit nanomolar level.
Keywords :
C5aR , Complement C5a , Antagonist , Aniline , tetrahydroquinoline
