【摘 要】
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A potential dual inhibitor(4) for exogenous absorption and endogenic synthesis of cholesterol was designed based on the conjugation of the β-lactam pharmacopho
【出 处】
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Chemical Research in Chinese Universities
论文部分内容阅读
A potential dual inhibitor(4) for exogenous absorption and endogenic synthesis of cholesterol was designed based on the conjugation of the β-lactam pharmacophore of ezetimibe and the δ-lactone pharmacophore of statins. The merger of ezetimibe and statin 4 was synthesized from p-hydroxybenzaldehyde through a ten-step route. 1H NMR analysis showed existence of four pairs of enantiomers(5.7:5.7:1:1, molar ratio). And compound 4 was found to lower total glucose(TG) level in rat serum via a high-cholesterol and high-fat feeding experiment.
A potential dual inhibitor (4) for exogenous absorption and endogenic synthesis of cholesterol was designed based on the conjugation of the β-lactam pharmacophore of ezetimibe and the δ-lactone pharmacophore of statins. The merger of ezetimibe and statin 4 was synthesized from p- 1H NMR analysis showed existence of four pairs of enantiomers (5.7: 5.7: 1: 1, molar ratio). And compound 4 was found to lower total glucose (TG) level in rat serum via a high -cholesterol and high-fat feeding experiment.
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