1028330-53-1Relevant articles and documents
Synthesis and characterization of 5,6,7,8-tetrahydroquinoline C5a receptor antagonists
Barbay, J. Kent,Gong, Yong,Buntinx, Mieke,Li, Jian,Claes, Concha,Hornby, Pamela J.,Van Lommen, Guy,Van Wauwe, Jean,He, Wei
, p. 2544 - 2548 (2008)
A novel series of substituted 2-aryl-5-amino-5,6,7,8-tetrahydroquinoline C5a receptor antagonists is reported. Synthetic routes were developed that allow the substituents on the tetrahydroquinoline core to be efficiently varied, facilitating determination of structure-activity relationships. Members of the series display high binding affinity for the C5a receptor and are potent functional antagonists.
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.