Structure-activity relationships of a series of novel topical corticosteroids

J Steroid Biochem. 1987;27(4-6):837-43. doi: 10.1016/0022-4731(87)90157-9.

Abstract

The 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.

Publication types

  • Comparative Study

MeSH terms

  • Administration, Topical
  • Adrenal Cortex Hormones / chemical synthesis
  • Adrenal Cortex Hormones / therapeutic use*
  • Animals
  • Anti-Inflammatory Agents*
  • Carboxylic Acids / chemical synthesis
  • Carboxylic Acids / therapeutic use
  • Chemical Phenomena
  • Chemistry
  • Croton Oil
  • Guinea Pigs
  • Inflammation / chemically induced
  • Inflammation / drug therapy
  • Mice
  • Psoriasis / drug therapy
  • Psoriasis / etiology
  • Structure-Activity Relationship
  • Tinea Versicolor / drug therapy

Substances

  • Adrenal Cortex Hormones
  • Anti-Inflammatory Agents
  • Carboxylic Acids
  • Croton Oil