Synthesis and Biological Evaluation of Ezetimibe Analogs as Possible Cholesterol Absorption Inhibitors
2011

Study of Ezetimibe Analogs for Cholesterol Absorption Inhibition

Sample size: 6 publication Evidence: moderate

Author Information

Author(s): Wang Yubin, Haiqian, Huang Wenlong, Zhang Huibin, Zhou Jinpei

Primary Institution: Nanjing University of Technology

Hypothesis

The introduction of amide groups and electron-deficient pyridine rings to Ezetimibe analogs will enhance their ability to inhibit cholesterol absorption.

Conclusion

Most of the synthesized Ezetimibe analogs showed comparable effects in lowering total cholesterol levels in serum.

Supporting Evidence

  • Eight new derivatives of 2-azetidinone were synthesized and evaluated for cholesterol absorption inhibition.
  • Most new compounds showed moderate effects in lowering total cholesterol in serum.
  • Compounds 3a and 3b significantly raised HDL-C levels.

Takeaway

The researchers made new versions of a cholesterol-lowering drug and found that many of them worked well to reduce cholesterol in hamsters.

Methodology

Eight new derivatives of 2-azetidinone were synthesized and tested for their ability to inhibit cholesterol absorption in hamsters.

Limitations

The study was limited to animal testing and the effects on humans are not yet known.

Participant Demographics

Cholesterol-fed hamsters were used for testing.

Statistical Information

P-Value

p<0.05

Statistical Significance

p<0.05

Digital Object Identifier (DOI)

10.2174/157018011795906776

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