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Bioorg Med Chem Lett. 2008 Jul 15;18(14):3852-5. doi: 10.1016/j.bmcl.2008.06.059. Epub 2008 Jun 20.

Design and optimization of aniline-substituted tetrahydroquinoline C5a receptor antagonists.

Author information

1
Johnson & Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA. ygong@prdus.jnj.com

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 IC(50) of selected analogs was optimized to the single-digit nanomolar level.

PMID:
18595693
DOI:
10.1016/j.bmcl.2008.06.059
[Indexed for MEDLINE]

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