Synthesis and pharmacology of anti-inflammatory steroidal antedrugs.
Synthesis and pharmacology of anti-inflammatory steroidal antedrugs.
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DOI：
10.1021/cr068203e
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发表时间：
2008-12
期刊：
影响因子：
62.1
通讯作者：
Lee, Henry J.
中科院分区：
文献类型：
--
作者：
Khan, M. Omar F.;Lee, Henry J.
本综述的目的是为了全面了解抗炎类固醇前药。前药的概念于1982年首次提出，此后，世界范围内的一些学术机构和一些制药行业正在这一领域进行积极的研究，以寻找更安全的治疗药物。尽管这一概念主要集中于发现更安全的局部抗炎类固醇，但其范围也扩大到其他治疗药物类别。最近的一篇评论简要概述了当前可用的前药发现的所有不同方法。由于人们对前药方法的兴趣日益浓厚以及类固醇化学的广泛性，本综述的重点集中在抗炎类固醇前药上。自 20 世纪 80 年代以来，在类固醇前体药物的化学合成和药理作用方面的研究工作决定了本文的广度。为了信息的完整性和一致性，还引用了历史资料和早期相关著作的参考文献。在简要介绍糖皮质激素治疗，特别是其临床应用和有害缺点以及早期药物化学努力克服这些缺点后，介绍了前药方法，概述了其基本原理、范围和成功。还解释了其他相关概念（例如前药）之间的界限。主要重点是所有化学类别的抗炎类固醇前药的合成方法及其药理活性，还有一节专门介绍前药。最后，为了反映前药概念的范围和未来，基于此概念开发的临床使用或在研药物已放在结束语之前。
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, 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 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.
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DOI：
10.1039/a908358h
发表时间：
2000-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1
影响因子：
--
作者：
Biggadike, K;Lynn, SM;Williamson, C
通讯作者：
Williamson, C
DOI：
10.1039/b200190j
发表时间：
2002-01-01
期刊：
JOURNAL OF THE CHEMICAL SOCIETY-PERKIN TRANSACTIONS 1
影响因子：
--
作者：
Angell, RM;Biggadike, K;Procopiou, PA
通讯作者：
Procopiou, PA
DOI：
10.1089/jop.1993.9.157
发表时间：
1993-06-01
期刊：
JOURNAL OF OCULAR PHARMACOLOGY
影响因子：
--
作者：
BARTLETT, JD;HORWITZ, B;HOWES, JF
通讯作者：
HOWES, JF
影响因子：
3.4
作者：
BODOR, N;VARGA, M
通讯作者：
VARGA, M
影响因子：
3.7
作者：
BODOR, N;MURAKAMI, T;WU, WM
通讯作者：
WU, WM