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- W2951800544 abstract "The synthesis and the in vitro pharmacological evaluation of a number of topical corticosteroid derivatives designed on the basis of the antedrug concept are reported. Three series of compounds were synthesized in which sulfur-containing amino acids were incorporated to the steroidal structure in the 21 position. Compounds of series 1 are diesters of cystine with the 21-hydroxyl groups of the corticosteroids, while series II and III contain 21-amino and 21-thio corticosteroid derivatives, respectively. The new compounds were less potent than the parent corticosteroids in vitro. The 21-yl-[9α-fluoro-11β, 17α-dihydroxy-16α-methyl-1,4-pregnadiene-3,20-dione]-S-acetylamino cysteine 13 was the most interesting compound of the series and is now under further evaluation. La synthèse et l'évaluation pharmacologique d'un certain nombre de dérivés corticoïdes conçus en accord avec le concept d'antedrug sont décrits. Trois séries de composés sont synthétisés dans lesquels des amino-acides soufrés sont incorporés en position 21 de la structure stéroïdienne. Les composés de la série 1 sont des diesters de la cystine avec le groupement hydroxyl en position 21, tandis que les séries II et III sont des amino-21 et thio-21 stéroïdes. Les nouveaux composés sont moins actifs in vitro que les stéroïdes de départ. Le composé21-yl-[9α-fluoro11β, 17α-dihydroxy-16α-methyl-1,4-pregnadiene-3,20-dione]-S-acétylamino cystéine 13 était le plus intéressant des trois séries et il est en cours d'études plus poussées." @default.
- W2951800544 created "2019-06-27" @default.
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- W2951800544 date "1991-12-01" @default.
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- W2951800544 title "Synthesis of new local anti-inflammatory thiosteroids based on antedrug concept" @default.
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- W2951800544 doi "https://doi.org/10.1016/0223-5234(91)90137-c" @default.
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