LailaImpex R&D Center, Unit-I, Phase-III, Jawahar Auto Nagar, Vijayawada 520 007, Andhra Pradesh, India.
Department of Pharmaceutical Chemistry, AU College of Pharmaceutical Sciences, Andhra University, Visakhapatnam 530 003, Andhra Pradesh, India.
Bioorg Chem. 2018 Oct;80:408-421. doi: 10.1016/j.bioorg.2018.06.015. Epub 2018 Jun 8.
A new series of diaryl heptanones (12a-q) were synthesized and their structures were confirmed by its H, C NMR and Mass spectral data. These analogs were evaluated for their anti-oxidant activity and potential to inhibit 5-lipoxygenase. Compounds 12k and 12o showed potent in vitro 5-lipoxygenase enzyme inhibitory activity with IC values of 22.2, 21.5 μM, which are comparable to curcumin (24.4 μM). Further they also have shown significant antioxidant activity. Molecular docking studies clearly showed correlation between binding energy and potency of these compounds.
我们合成了一系列新的二芳基庚烷（12a-q），并通过其氢谱、碳谱和质谱数据确定了它们的结构。这些类似物的抗氧化活性和抑制 5-脂氧合酶的潜力进行了评估。化合物 12k 和 12o 对 5-脂氧合酶表现出较强的体外抑制活性，IC 值分别为 22.2、21.5 μM，与姜黄素（24.4 μM）相当。此外，它们还表现出显著的抗氧化活性。分子对接研究清楚地表明了这些化合物的结合能和效力之间的相关性。
