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Letters in Drug Design & Discovery


ISSN (Print): 1570-1808
ISSN (Online): 1875-628X

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

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

Volume 8 , Issue 6 , 2011

Page: [500 - 505] Pages: 6

DOI: 10.2174/157018011795906776

Price: $65


In order to investigate the SAR of Ezetimibe analogs for cholesterol absorption inhibitions, amide group and electron-deficient pyridine ring were introduced to the C-(3) carbon chain of Ezetimibe. Eight new derivatives of the 2- azetidinone cholesterol absorption inhibitors have been synthesized, and all of them were enantiomerically pure. All the new compounds were evaluated for their activity to inhibit cholesterol absorption in hamsters, and most of them showed comparable effects in lowering the levels of total cholesterol in the serum.

Keywords: 2-Azetidinone derivatives, Enantiomerically pure, Cholesterol absorption inhibition, Ezetimibe Analogs, Cholesterol, SAR, Ezetimibe(1), C-(3) sidechain, N-aryl ring, bio isosteric, β-lactam ring, CHD, serum

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