Studies on topical antiinflammatory corticosteroids. I. Syntheses and vasoconstrictive activities of 11.BETA.,17.ALPHA.,21-trihydroxy-6.ALPHA.-methyl-1,4-pregnadiene-3,20-dione 17-ester and 17,21-diester derivatives.
- 1 January 1985
- journal article
- research article
- Published by Pharmaceutical Society of Japan in CHEMICAL & PHARMACEUTICAL BULLETIN
- Vol. 33 (5) , 1889-1898
- https://doi.org/10.1248/cpb.33.1889
Abstract
Seven 17-ester and thiry-eight 17,21-diester compounds of 11.beta.,17.alpha.,21-trihydroxy-6.alpha.-methyl-1,4-pregnadiene-3,20-dione (6.alpha.-methylprednisolone(1) were synthesized and 38 selected compounds were tested for vasoconstrictive activity in humans. They were generally more active than the mother compound (1). In particular, the activities of 10 compounds were equal to or greater than that of 9.alpha.-fluoro-11.beta.,21-dihydroxy-16.beta.-methyl-17.alpha.-valeryloxy-1,4-pregnadiene-3,20-dione (betamethasone 17-valerate, BV). The activities of 21-methoxyacetate compounds were potent. The structure-activity relationship is discussed.This publication has 4 references indexed in Scilit:
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