PubMed:3695507 JSONTXT

{"project":"Inflammaging","denotations":[{"id":"T1","span":{"begin":0,"end":78},"obj":"Sentence"},{"id":"T2","span":{"begin":79,"end":183},"obj":"Sentence"},{"id":"T3","span":{"begin":184,"end":329},"obj":"Sentence"},{"id":"T4","span":{"begin":330,"end":474},"obj":"Sentence"},{"id":"T5","span":{"begin":475,"end":551},"obj":"Sentence"},{"id":"T6","span":{"begin":552,"end":714},"obj":"Sentence"},{"id":"T7","span":{"begin":715,"end":792},"obj":"Sentence"},{"id":"T8","span":{"begin":793,"end":873},"obj":"Sentence"},{"id":"T9","span":{"begin":874,"end":992},"obj":"Sentence"},{"id":"T10","span":{"begin":993,"end":1107},"obj":"Sentence"},{"id":"T1","span":{"begin":0,"end":78},"obj":"Sentence"},{"id":"T2","span":{"begin":79,"end":183},"obj":"Sentence"},{"id":"T3","span":{"begin":184,"end":329},"obj":"Sentence"},{"id":"T4","span":{"begin":330,"end":474},"obj":"Sentence"},{"id":"T5","span":{"begin":475,"end":551},"obj":"Sentence"},{"id":"T6","span":{"begin":552,"end":714},"obj":"Sentence"},{"id":"T7","span":{"begin":715,"end":792},"obj":"Sentence"},{"id":"T8","span":{"begin":793,"end":873},"obj":"Sentence"},{"id":"T9","span":{"begin":874,"end":992},"obj":"Sentence"},{"id":"T10","span":{"begin":993,"end":1107},"obj":"Sentence"}],"text":"Structure-activity relationships of a series of novel topical corticosteroids.\nThe effect of various heteroaroyl groups in the 17-position of topical corticosteroids has been studied. The corticosteroids esterified at C17 were of 9 alpha,11 beta-dichloro, 9 alpha-chloro 11 beta-hydroxy and 9 alpha-fluoro 11 beta-hydroxy series. Among the 17-acyl groups 2'-furoates were most extensively investigated, although 2'-thenoates, 3'-thenoates and 3'-furoates were also examined. Many of these esters exhibited enhanced topical anti-inflammatory potencies. The most potent compounds investigated were the 21-chloro 17(2'-furoates) either in the 9 alpha,11 beta-dichloro, or in the 9 alpha-chloro 11 beta-hydroxy series. These compounds were at least 6 times as potent as betamethasone 17-valerate. Among 16-substituents studied 16 alpha-methyl compounds had the highest potency. Topical anti-inflammatory potencies were determined by using a 5-day modification of the croton oil ear assay in mice. The more potent compounds were also evaluated in the P. ovale induced chronic psoriaform lesion in the guinea-pig."}