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2-氮杂环丁烷酮衍生物:胆固醇吸收抑制剂的设计、合成与评价

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

作者信息

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

机构信息

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

出版信息

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

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.

摘要

已合成了14种新型2-氮杂环丁烷酮胆固醇吸收抑制剂衍生物,其中3种为对映体纯品。对所有新化合物进行了抑制大鼠胆固醇吸收活性的评估,大多数化合物在降低血清总胆固醇水平方面表现出相当的效果。

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