| Autor: |
Gong Y; Johnson & Johnson Pharmaceutical Research and Development, Spring House, PA 19477-0776, USA. ygong@prdus.jnj.com, Barbay JK, Buntinx M, Li J, Wauwe JV, Claes C, Lommen GV, Hornby PJ, He W |
| Jazyk: |
angličtina |
| Zdroj: |
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2008 Jul 15; Vol. 18 (14), pp. 3852-5. Date of Electronic Publication: 2008 Jun 20. |
| DOI: |
10.1016/j.bmcl.2008.06.059 |
| Abstrakt: |
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. |
| Databáze: |
MEDLINE |
| Externí odkaz: |
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