99598-45-5Relevant academic research and scientific papers
Studies on topical antiinflammatory corticosteroids. I. Syntheses and vasoconstrictive activities of 11β,17α,21-trihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione 17-ester and 17,21-diester derivatives
Sugai,Okazaki,Kajiwara,Kanbara,Naito,Yoshida,Akaboshi,Ikegami,Kamano
, p. 1889 - 1898 (1985)
Seven 17-ester and thirty-eight 17,21-diester compounds (3 and 4) of 11β,17α,21-trihydroxy-6α-methyl-1,4-pregnadiene-3,20-dione (6α-methylprednisolone, 1) were synthesized and thirty-eight selected compounds were tested for vasoconstrictive activity in humans. Except for 4g1 and 4g2, they were more active than the mother compound (1). In particular, the activities of ten compounds (3b-g, 4b9,10, 4c2,3, and 4c6) were equal to or greater than that of 9α-fluoro-11β,21-dihydroxy-16β-methyl-17α-valeryloxy-1,4-pregnadiene-3 ,20-dione (betamethasone 17-valerate, BV). The activities of 21-methoxyacetate compounds (4b9, 4c6 and 4d5) were potent. The structure-activity relationship is discussed.
