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Recent advances in the structure-activity relationships of substituted corticosteroids.
TLDR
Potency of 9α-unsubstituted corticosteroids was found to be increased by 5–8 times on introduction of the 6-azido-6-ene group and the potency substantially unchanged in the presence of a 1,2-double bond. Expand
Synthesis and structure-activity studies of a series of 7 alpha-halogeno corticosteroids.
TLDR
The preparation and topical antiinflammatory potencies of a series of 7 alpha-halogeno-16-substituted-prednisolone derivatives are described, where the greatest effect of a 7alpha-halogens was observed in the 16 alpha-methylprednisolione series, where 7Alpha-chloro and7 alpha-bromo substitution increased potency 2.5- to 3. Expand
Selective effects of 7 alpha-halogeno substitution on corticosteroid activity: Sch 22219 and Sch 23409.
TLDR
Both compounds possess enhanced topical antiinflammatory potency, with the potential for reduced side effects in man, and were at least equivalent to the most potent comparison corticosteroids in topical anti inflammatory activity. Expand
Synthesis and structure-activity relationships in a novel series of topically active corticosteroids.
TLDR
The influence of 7α-halogeno substitution on topical anti-inflammatory potency was studied in a series of prednisolone derivatives and the greatest effect was observed in the 16α-methylprednisolones series, where both 6,7-dehydro and 7 α-bromo substitution yielded compounds equivalent in potency to betamethasone dipropionate. Expand
The influence of esterification on the topical antiinflammatory activity of 7 alpha-chloro- and 7 alpha-bromo-16 alpha-methylprednisolones.
TLDR
Among diesters of 7-halogenocorticosteroids, structure seems to be more important for topical potency than lipophilicity. Expand
Synthesis and topical antiinflammatory potencies of a series of 6-keto- and delta 6-6-acyloxybetamethasone derivatives.
TLDR
6-keto- and delta 6-6-acyloxybetamethasone esters were synthesized, and tested for topical antiinflammatory potency using a modification of the Tonelli croton ear assay, leading to retention of topical anti inflammatory potencies when compared to the corresponding 6-desoxycorticoids. Expand
A novel class of potent topical antiinflammatory agents: 17-benzoylated, 7 alpha-halogeno substituted corticosteroids.
TLDR
Surprisingly, little potency enhancement due to 7 alpha-halogenation was discerned in the 16 beta-methylprednisolone series, and structurally novel corticosteroids with topical potencies significantly higher than those of the corresponding 17,21-dipropionate analogs were found. Expand
RECENT ADVANCES IN THE STRUCTURE–ACTIVITY RELATIONSHIPS OF SUBSTITUTED CORTICOSTEROIDS
The influence of the 6-azido-6-ene grouping on corticosteroid activity has been studied. The 6-azido-6-ene-corticosteroids were synthesized by reaction of the methanesulfonate esters ofExpand
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