Synthesis and Pharmacology of Anti-Inflammatory Steroidal Antedrugs

摘要

The purpose of this review is to give a comprehensive understanding about anti-inflammatory steroidal antedrugs The concept of antedrug first came into light in 1982, andsince 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 on the discovery of safer topical anti-inflammatory steroids, the scope has broadened involving other therapeutic drug classes as well. A recent review has outlined briefly 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 have been concentrated on anti-inflammatory steroidal antedrugs. The research efforts since the 1980s in the chemical synthesis and pharmacological actions of the steroidal antedrugs have dictated the breadth of this article For the sake of completeness of information and consistency, historical materials and references to earlier relevant works have 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 has also been devoted to pro-antedrugs. 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 have been placed before the concluding remarks.