4-CF3-ezetimibe analogs: design,synthesis, and biological evaluation of cholesterol absorption inhibitions |
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| Authors: | Yingle Liu Jun-Ling Chen Gai-Hong Wang Peng Sun Heyao Huang Feng-Ling Qing |
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| Affiliation: | 1. College of Chemistry, Chemical Engineering and Biotechnology, Donghua University, 2999 North Renmin Lu, Shanghai 201620, China;2. Key Laboratory of Organofluorine Chemistry, Shanghai Institute of Organic Chemistry, Chinese Academy of Science, 345 Lingling Lu, Shanghai 200032, China;3. Shanghai Institute of Materia Medica, Chinese Academy of Sciences, 555 Zucongzhi Lu, Shanghai 201203, China |
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| Abstract: | On the purpose of looking for better cholesterol absorption inhibitors, several trifluoromethyl substituted ezetimibe analogs 1a–d were designed and synthesized. The key steps in the synthesis of these optically pure trans-4-CF3-β-lactams include chiral auxiliary induced asymmetric hydrogenation and substrate controlled stereoselective alkylation. The inhibitory activities of these target compounds were evaluated on the cholesterol absorption in Caco-2 cells. The result showed that the inhibitory activity of compound 1a was comparable to ezetimibe. |
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| Keywords: | Ezetimibe Cholesterol β-Lactam Trifluoromethyl Asymmetric hydrogention |
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