| Autor: |
Clark, M. P., Laughlin, S. K., Laufersweiler, M. J., Bookland, R. G., Brugel, T. A., Golebiowski, A., Sabat, M. P., Townes, J. A., VanRens, J. C., Djung, J. F., Natchus, M. G., De, B., Hsieh, L. C., Xu, S. C., Walter, R. L., Mekel, M. J., Heitmeyer, S. A., Brown, K. K., Juergens, K., Taiwo, Y. O., Janusz, M. J. |
| Zdroj: |
Journal of Medicinal Chemistry; May 2004, Vol. 47 Issue: 11 p2724-2727, 4p |
| Abstrakt: |
2-Aryl-3-pyrimidinyl based tumor necrosis factor-α (TNF-α) inhibitors, which contain a novel bicyclic pyrazolone core, are described. Many showed low-nanomolar activity against lipopolysaccharide-induced TNF-α production in monocytic cells. Secondary screening data are presented for the pyrimidinyl bicyclic pyrazolones. Several of these analogues showed good oral bioavailability in rat and efficacy in the rat iodoacetate in vivo model. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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