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Synthesis and Bioactivities of 2-Azetidinone Derivatives as Cholesterol Absorption Inhibitors

[ Vol. 7 , Issue. 6 ]

Author(s):

Yubin Wang, Hai Qian, Jinpei Zhou, Huibin Zhang, Jianfeng Ji and Wenlong Huang   Pages 534 - 542 ( 9 )

Abstract:


Twenty-four 2-azetidinone derivatives have been designed and synthesized as cholesterol absorption inhibitors. All new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed considerable effects in lowering the levels of total cholesterol in the serum, especially compound 2d, 4a, 4f, 4i and 4j.

Keywords:

2-Azetidinones, cholesterol absorption inhibitor, synthesis, bioactivities, hamsters, cardiovascular research, coronary heart disease (CHD), exogenous pathways, 3-methylglutaryl, 3-hydroxy

Affiliation:

Center of Drug Discovery, China Pharmaceutical University, 24 Tongjiaxiang, Nanjing 210009, China.



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