CRCU

Chemical Research in Chinese Universities ›› 2011, Vol. 27 ›› Issue (2): 232-236.

• Articles • Previous Articles     Next Articles

Merger of Ezetimibe and Statin: a Potential Dual Inhibitor

HE Xing-lian1, XU Xian-xiu3, ZHENG Lian-you1 and BAI Xu1,2*   

  1. 1. Center for Combinatorial Chemistry and Drug Discovery, School of Pharmaceutical Sciences, Jilin University, Changchun 130021, P. R. China;
    2. College of Chemistry, Jilin University, Changchun 130012, P. R. China;
    3. College of Chemistry, Northeast Normal University, Changchun 130024, P. R. China
  • Received:2010-01-29 Revised:2010-04-06 Online:2011-03-25 Published:2011-03-09
  • Contact: BAI Xu E-mail:xbai@jlu.edu.cn
  • Supported by:

    Supported by the Grant from the Bureau of Science and Technology of Changchun City, China(No.2005132).

PDF (PC)

Cited

3

Abstract: A potential dual inhibitor(4) for exogenous absorption and endogenic synthesis of cholesterol was designed based on the conjugation of the β-lactam pharmacophore of ezetimibe and the δ-lactone pharmacophore of statins. The merger of ezetimibe and statin 4 was synthesized from p-hydroxybenzaldehyde through a ten-step route. 1H NMR analysis showed existence of four pairs of enantiomers(5.7:5.7:1:1, molar ratio). And compound 4 was found to lower total glucose(TG) level in rat serum via a high-cholesterol and high-fat feeding experiment.

Key words: Multi-target drug, Ezetimibe, Statin