Synthesis and Topical Antiinflamatory Activity of Some Steroidal Isoxazolidines

DOI: 10.1021/jm00354a020

Source and publish data:

Journal of Medicinal Chemistry p. 1492 - 1495 (1982)

Update date:2022-08-04

Topics:

Authors:

Green, Michael J.

Tiberi, Robert L.

Friary, Richard

Lutsky, Barry N.

Berkenkoph, Joseph

et al. et al.

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Article abstract of DOI:10.1021/jm00354a020

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 <16α,17α-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 compound tested.The hexacyclic adduct 20 was inactive in this assay.

Full text of DOI:10.1021/jm00354a020

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