Synthesis and Topical Antiinflamatory Activity of Some Steroidal Isoxazolidines

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.