1046488-98-5Relevant articles and documents
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
Gong, Yong,Barbay, J. Kent,Buntinx, Mieke,Li, Jian,Wauwe, Jean Van,Claes, Concha,Lommen, Guy Van,Hornby, Pamela J.,He, Wei
scheme or table, p. 3852 - 3855 (2009/04/06)
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.