Synthesis and topical antiinflammatory activity of some steroidal [16. alpha., 17. alpha.-d]-isoxazolidines

…, R Friary, BN Lutsky, J Berkenkoph…

文献索引：Green, Michael J.; Tiberi, Robert L.; Friary, Richard; Lutsky, Barry N.; Berkenkoph, Joseph; et al. Journal of Medicinal Chemistry, 1982 , vol. 25, # 12 p. 1492 - 1495

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被引用次数: 32

摘要

1, 3-Dipolar cycloaddition of N-methylnitrone, N-benzylnitrone, and pyrroline N-oxide to 1, 4, 16-pregnatriene-3, 20-diones is described. In each case only [16a, l7a-d] isoxazolidines were isolated. The pentacyclic adducts 16-19 were active topical antiinflammatory agents in mice, with 18 being more potent than any of the standard compounds tested. The hexacyclic adduct 20 was inactive in this assay.