2-Azetidinone derivatives: design, synthesis and evaluation of cholesterol absorption inhibitors

Yubin Wang; Huibin Zhang; Wenlong Huang; Jing Kong; Jinpei Zhou; Beibei Zhang

doi:10.1016/j.ejmech.2008.09.033

2-Azetidinone derivatives: design, synthesis and evaluation of cholesterol absorption inhibitors

Eur J Med Chem. 2009 Apr;44(4):1638-43. doi: 10.1016/j.ejmech.2008.09.033. Epub 2008 Oct 7.

Authors

Yubin Wang¹, Huibin Zhang, Wenlong Huang, Jing Kong, Jinpei Zhou, Beibei Zhang

Affiliation

¹ New Drug Research Center, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.

PMID: 18990470
DOI: 10.1016/j.ejmech.2008.09.033

Abstract

Fourteen new derivatives of the 2-azetidinone cholesterol absorption inhibitors have been synthesized, and three of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in rats, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.

Publication types

Research Support, Non-U.S. Gov't

MeSH terms

Absorption / drug effects
Animals
Azetidines / chemical synthesis
Azetidines / chemistry*
Azetidines / pharmacology*
Cholesterol / metabolism*
Cricetinae
Drug Design*
Male

Substances

2-azetidinone
Azetidines
Cholesterol