查耳酮及其吡唑衍生物的合成及血管紧张素转化酶（ACE）抑制活性。
The synthesis and angiotensin converting enzyme (ACE) inhibitory activity of chalcones and their pyrazole derivatives.
机构信息
Department of Pharmaceutical Sciences, Faculty of Pharmacy, Nutrition and Health Sciences, University of Calabria, Rende (CS), Italy.
出版信息
Bioorg Med Chem Lett. 2010 Mar 15;20(6):1990-3. doi: 10.1016/j.bmcl.2010.01.113. Epub 2010 Jan 25.
A series of chalcones (1-9) and pyrazoles (10-18) was prepared to investigate their potential activity as Angiotensin I-Converting Enzyme (ACE) inhibitors. Their structures were verified by elemental analysis, UV, IR, MS, (1)H NMR, (13)C NMR, and 2D NMR experiments. Among tested compounds, chalcone 7 exerted the highest activity with an IC(50) value of 0.219 mM, while the most potent pyrazole was 15 (IC(50) value of 0.213 mM).
我们合成了一系列查耳酮（1-9）和吡唑（10-18）衍生物，以研究它们作为血管紧张素转化酶（ACE）抑制剂的潜力。通过元素分析、紫外光谱、红外光谱、质谱、（1）H NMR、（13）C NMR 和二维 NMR 实验对它们的结构进行了验证。在所测试的化合物中，查尔酮 7 的活性最高，IC（50）值为 0.219mM，而最有效的吡唑衍生物是 15（IC（50）值为 0.213mM）。
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