| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 1364958 | Bioorganic & Medicinal Chemistry Letters | 2008 | 4 Pages |
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.
Graphical abstractA series of aniline-substituted tetrahydroquinoline C5aR antagonists with distinct structure-activity relationships are presented.Figure optionsDownload full-size imageDownload as PowerPoint slide
Related Topics
Physical Sciences and Engineering
Chemistry
Organic Chemistry
Authors
Yong Gong, J. Kent Barbay, Mieke Buntinx, Jian Li, Jean Van Wauwe, Concha Claes, Guy Van Lommen, Pamela J. Hornby, Wei He,