| Autor: |
Daines, R. A., Chambers, P. A., Foley, J. J., Griswold, D. E., Kingsbury, W. D., Martin, L. D., Schmidt, D. B., Sham, K. K. C., Sarau, H. M. |
| Zdroj: |
Journal of Medicinal Chemistry; September 13, 1996, Vol. 39 Issue: 19 p3837-3841, 5p |
| Abstrakt: |
An extensive structure−activity study based around the high-affinity leukotriene B4 (LTB4) receptor antagonist SB 201146 (1) led to the identification of (E)-3-[6-[[(2,6-dichlorophenyl)thio]methyl]-3-(2-phenylethoxy)-2-pyridinyl]-2-propenoic acid (3). This compound displays high affinity for the human neutrophil LTB4 receptor (Ki = 0.78 nM), blocks LTB4-induced Ca2+ mobilization with an IC50 of 6.6 ± 1.5 nM, and demonstrates potent oral and topical antiinflammatory activity in a murine model of dermal inflammation. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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