Synthesis and Pharmacology of Anti-inflammatory Steroidal Antedrugs

Document Type


Publication Date

Winter 12-2008


The purpose of this review is to give a comprehensive understanding about the anti-inflammatory steroidal antedrugs. The concept of antedrug first came into light in 1982 and since then a few academic institutions and some pharmaceutical industries worldwide are performing active research in this avenue in search of safer therapeutic agents. Although the concept primarily focused to the discovery of safer topical anti-inflammatory steroids, the scopes has broadened involving other therapeutic drug classes as well. A recent review has outlined briefly on all different currently available approaches of antedrug discovery. Because of the increasing interests on antedrug approach and vastness of steroid chemistry, the focuses of the present review had been concentrated on anti-inflammatory steroidal antedrugs. The research efforts since 1980s in the chemical synthesis and pharmacological actions of the steroidal antedrugs have dictated the breadth of this article. For the sake of the completeness of information and consistency, historical materials and references to earlier relevant works has also been cited. After a brief introduction about the glucocorticoid therapy, especially their clinical applications and deleterious shortcomings and earlier medicinal chemical efforts to overcome those shortcomings, the antedrug approach is introduced outlining the rationale, scopes and successes. Borderline between the other related concepts such as prodrug has also been explained. The synthetic approaches of all chemical classes of anti-inflammatory steroidal antedrugs and their pharmacological activities have been the main emphasis and a section on pro-antedrugs has also been devoted. Finally, to reflect the scopes and future of the concept of antedrug, drugs in clinical use or in pipeline that are developed based on this concept has been placed before the concluding remarks.


The version of record is available from the publisher at Copyright © 2008 American Chemical Society.