| Literature DB >> 18595693 |
Yong Gong1, J Kent Barbay, Mieke Buntinx, Jian Li, Jean Van Wauwe, Concha Claes, Guy Van Lommen, Pamela J Hornby, Wei He.
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.Entities:
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Year: 2008 PMID： 18595693 DOI： 10.1016/j.bmcl.2008.06.059
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823