| Autor: |
Hays, S. J., Caprathe, B. W., Gilmore, J. L., Amin, N., Emmerling, M. R., Michael, W., Nadimpalli, R., Nath, R., Raser, K. J., Stafford, D., Watson, D., Wang, K., Jaen, J. C. |
| Zdroj: |
Journal of Medicinal Chemistry; March 26, 1998, Vol. 41 Issue: 7 p1060-1067, 8p |
| Abstrakt: |
A series of 2-amino-4H-3,1-benzoxazin-4-ones have been synthesized and evaluated as inhibitors of the complement enzyme C1r. C1r is a serine protease at the beginning of the complement cascade, and complement activation by β-amyloid may represent a major contributing pathway to the neuropathology of Alzheimer's disease. Compounds such as 7-chloro-2-[(2-iodophenyl)amino]benz[d][1,3]oxazin-4-one (32) and 7-methyl-2-[(2-iodophenyl)amino]benz[d][1,3]oxazin-4-one (37) show improved potency compared to the reference compound FUT-175. Many of these active compounds also possess increased selectivity for C1r compared to trypsin and enhanced hydrolytic stability relative to 2-(2-iodophenyl)-4H-3,1-benzoxazin-4-one (1). |
| Databáze: |
Supplemental Index |
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