Title of article
Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists
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 ,
Issue Information
روزنامه با شماره پیاپی سال 2008
Pages
4
From page
3852
To page
3855
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
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2008
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
799667
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