迈向化学预防剂的开发。第1部分：一类新型2,5-二取代二氧杂环烷烃的设计、合成及抗炎活性

Toward the development of chemoprevention agents. Part 1: Design, synthesis, and anti-inflammatory activities of a new class of 2,5-disubstituted-dioxacycloalkanes.

作者信息

Gu Keli, Bi Lanrong, Zhao Ming, Wang Chao, Ju Jingfang, Peng Shiqi

机构信息

College of Pharmaceutical Sciences, Capital University of Medical Sciences, Beijing 100054, PR China.

出版信息

Bioorg Med Chem. 2007 Jul 15;15(14):4775-99. doi: 10.1016/j.bmc.2007.05.013. Epub 2007 May 6.

DOI:10.1016/j.bmc.2007.05.013

PMID:17512740

Abstract

A new class of 2,5-disubstituted-dioxacycloalkanes were designed and synthesized via stereoselective synthetic method as cancer chemoprevention agents. The anti-inflammatory activities of these compounds were tested using the xylene-induced mouse ear edema model. Some of these compounds exhibited comparable or better anti-inflammatory activities than that of aspirin suggesting that they can be further developed as potential anti-inflammatory drug lead compounds. In addition, treatment of these anti-inflammatory agents did not prolong tail bleeding time in mice. The structure/activity relationships were also analyzed among these compounds.

摘要

通过立体选择性合成方法设计并合成了一类新型的2,5-二取代二氧杂环烷烃作为癌症化学预防剂。使用二甲苯诱导的小鼠耳肿胀模型测试了这些化合物的抗炎活性。其中一些化合物表现出与阿司匹林相当或更好的抗炎活性，这表明它们可以作为潜在的抗炎药物先导化合物进一步开发。此外，这些抗炎剂的处理并未延长小鼠的尾部出血时间。还分析了这些化合物之间的构效关系。

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