Chemical and Pharmaceutical Bulletin p. 692 - 697 (1990)
Update date:2022-08-04
Topics:
Mitsukuchi
Ikemoto
Taguchi
Higuchi
Abe
Yasui
Hatayama
As part of our search for new topical antiinflammatory agents, a series of corticosteroid 17-(alkylthio)- and methoxyalkanoate derivatives was prepared and tested for vasoconstrictive activities. Several compounds were proved to have activity superior or comparable to that of 9α-fluoro-11β,21-dihydroxy-16β-methyl-17α-valeryloxy-1,4- pregnadiene-3,20-dione (betamethasone 17-valerate, BV). Among these compounds, 21-chloro-11β-hydroxy-17α-(methylthio)acetoxy-4- pregnene-3,20-dione (5Aa) was found to have the most potent activity, being more active than BV. The structure-activity relationships of the series revealed that introduction of a (methylthio)acetate function into the 17-position as well as the 21-position of corticosteroids was effective for enhancing the topical antiinflammatory activity.
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Doi:10.1016/0022-328X(84)85065-2
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