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- W2326420185 abstract "17-Methoxyacetate (3a) and 17-(methylthio)acetate (3b) of 11β, 17α, 21-trihydroxy-6α-methyl-1, 4-pregnadiene-3, 20-dione (6α-methylprednisolone, 1) and their 21-esters (4a and 4b) were synthesized and tested for vasoconstrictive activities. The activities of the 17-(methylthio)acetate derivatives (3b and 4b) were more potent than those of the corresponding 17-methoxyacetates (3a and 4a). The activities of 3b, 4a2, 4b1-4 and 4b5 were equivalent to that of 9α-fluoro-11β, 21-dihydroxy-16β-methyl-17α-valeroyloxy-1, 4-pregnadiene-3, 20-dione (betamethasone 17-valerate, BV). The reaction of 6α-methylprednisolone (1) with triethyl orthomethoxyacetate afforded a stereoisomeric mixture of 6α-methylprednisolone 17, 21-cyclic ortho esters (2aA and 2aB) in a ratio of 22 : 78, while the reaction of 1 with triethyl ortho(methylthio)acetate resulted in the formation of a single isomer (2bB) of the isomeric 17, 21-cyclic ortho esters (2b)." @default.
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- W2326420185 date "1986-01-01" @default.
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- W2326420185 title "Studies on topical antiinflammatory corticosteroids. II Synthesis and vasoconstrictive activity of 11.BETA.,17.ALPHA.,21-trihydroxy-6.ALPHA.-methyl-1,4-pregnadiene-3,20-dione 17-methoxy- and (methylthio)acetates." @default.
- W2326420185 doi "https://doi.org/10.1248/cpb.34.1607" @default.
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