| Autor: |
Janusz, J. M., Young, P. A., Scherz, M. W., Enzweiler, K., Wu, L. I., Gan, L., Pikul, S., McDow-Dunham, K. L., Johnson, C. R., Senanayake, C. B., Kellstein, D. E., Green, S. A., Tulich, J. L., Rosario-Jansen, T., Magrisso, I. J., Wehmeyer, K. R., Kuhlenbeck, D. L., Eichhold, T. H., Dobson, R. L. M. |
| Zdroj: |
Journal of Medicinal Chemistry; March 26, 1998, Vol. 41 Issue: 7 p1124-1137, 14p |
| Abstrakt: |
A series of 5-keto-substituted 7-tert-butyl-2,3-dihydro-3,3-dimethylbenzofurans (DHDMBFs) were found to be nonsteroidal antiinflammatory and analgesic agents. These compounds are inhibitors of 5-lipoxygenase (5-LOX) and cyclooxygenase (COX) with selectivity for the COX-2 isoform. A series of analogues were prepared to investigate the scope of this lead. Five ketone side chains from active DHDMBFs were used to investigate the effects of changes in the DHDMBF core: the size and identity of the heterocycle and the substituent requirements of the heterocycle and phenyl ring. Biological testing showed that a variety of structural changes can be accommodated, but no structure was clearly superior to the DHDMBF structure. |
| Databáze: |
Supplemental Index |
| Externí odkaz: |
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