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 IC(50) of selected analogs was optimized to the single-digit nanomolar level.
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| http://dx.doi.org/10.1016/j.bmcl.2008.06.059 | DOI Listing |
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Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists.
Bioorg Med Chem Lett
July 2008
Johnson & Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA.
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.
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