有机化学 ›› 2013, Vol. 33 ›› Issue (08): 1674-1685.DOI: 10.6023/cjoc201212050 上一篇    下一篇

综述与进展

罗非昔布及其衍生物合成研究进展

刘改枝a, 韩德恩a, 王鹏b, 刘宏民b   

  1. a 河南中医学院药学院 郑州 450046;
    b 郑州大学药学院 郑州 450001
  • 收稿日期:2012-12-30 修回日期:2013-02-05 发布日期:2013-02-22
  • 通讯作者: 刘改枝, 刘宏民 E-mail:liugaizhi@126.com;liuhm@zzu.edu.cn
  • 基金资助:

    河南中医学院博士基金(No. BSJJ2010-03)资助项目.

Synthesis Research Progress of Rofecoxib and Its Derivatives

Liu Gaizhia, Han Deena, Wang Pengb, Liu Hongminb   

  1. a Henan University of TCM, Zhengzhou 450046;
    b School of Pharmaceutical Science, Zhengzhou University, Zhengzhou 450001
  • Received:2012-12-30 Revised:2013-02-05 Published:2013-02-22
  • Supported by:

    Project supported by the Doctoral Research Foundation of Henan University of Traditional Chinese Medicine (No. BSJJ2010-03).

罗非昔布是一种新型非甾体抗炎药, 是环氧化酶抑制剂的代表性药物, 服用罗非昔布会增加患心脏病或中风的危险. 虽然罗非昔布曾由于心血管安全风险而撤市, 但其优异的镇痛抗炎活性仍然具有很大的研究价值和广阔的应用前景, 因此以罗非昔布为先导寻找具有更高药理活性或更低毒副作用的罗非昔布衍生物一度成为研究热点. 综述了罗非昔布及其衍生物的研究进展, 包括罗非昔布合成工艺的研究, 罗非昔布衍生物的合成.

关键词: 罗非昔布, 衍生物, 合成, 研究进展

Rofecoxib is a novel non-steroidal anti-inflammatory drug, which is the representative of cyclooxygenase inhibitor. Taking rofecoxib would increase the risk of heart attack or stroke risk. Although rofecoxib withdrawal from the market due to cardiovascular risk, but its excellent analgesic and anti-inflammatory activity still has great research value and broad application prospect. Therefore, rofecoxib as a lead compound, has become a focus of research, from which researchers try to find good activity and little side effects rofecoxib derivatives. The research progress of rofecoxib and its derivatives is reviewed, including synthesis of rofecoxib and its derivatives.

Key words: rofecoxib, derivative, synthesis, research progress