1028331-11-4Relevant academic research and scientific papers
SUBSTITUTED 5,6,7,8-TETRAHYDROQUINOLINE DERIVATIVES, COMPOSITIONS, AND METHODS OF USE THEREOF
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Page/Page column 27, (2009/03/07)
Substituted 5,6,7,8-tetrahydroquinoline derivatives, which are C5a receptor modulators, compositions containing these derivatives, and methods of their use for the prevention and treatment of conditions, including, inter alia, immune and inflammatory diseases and conditions, are disclosed.
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 (2008/12/21)
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.
