杨璐, 史行, 李云兰, 陈曦, 牛思青, 乔晓枝, 买佳琪, 李青山. 新型含异丁基苯甲酮类化合物的合成及抗炎活性的初步研究J. 药学学报, 2018,53(2): 256-262. doi: 10.16438/j.0513-4870.2017-1224
引用本文: 杨璐, 史行, 李云兰, 陈曦, 牛思青, 乔晓枝, 买佳琪, 李青山. 新型含异丁基苯甲酮类化合物的合成及抗炎活性的初步研究J. 药学学报, 2018,53(2): 256-262. doi: 10.16438/j.0513-4870.2017-1224
YANG Lu, SHI Hang, LI Yun-lan, CHEN Xi, NIU Si-qing, QIAO Xiao-zhi, MAI Jia-qi, LI Qing-shan. Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivativesJ. Acta Pharmaceutica Sinica, 2018,53(2): 256-262. doi: 10.16438/j.0513-4870.2017-1224
Citation: YANG Lu, SHI Hang, LI Yun-lan, CHEN Xi, NIU Si-qing, QIAO Xiao-zhi, MAI Jia-qi, LI Qing-shan. Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivativesJ. Acta Pharmaceutica Sinica, 2018,53(2): 256-262. doi: 10.16438/j.0513-4870.2017-1224

新型含异丁基苯甲酮类化合物的合成及抗炎活性的初步研究

Synthesis and anti-inflammatory activity of novel isobutyl benzophenone derivatives

  • 摘要: 通过傅克酰基化反应、黄鸣龙还原反应合成了20个目标化合物,并通过LPS诱导的小鼠巨噬细胞RAW264.7炎症模型测定目标化合物对细胞上清液中NO的抑制作用并探讨了构效关系。合成的20个目标化合物全部为新化合物,其结构经ESI-MS、1H NMR和13C NMR确认。体外活性实验表明,有18个目标化合物在浓度为40 μmol·L-1时有一定的抗炎作用,其中以9a8b7c9c表现出较强的抗炎活性,7c9c的IC50与阳性对照药布洛芬相当。

     

    Abstract: Twenty target compounds were synthesized by the reduction reaction of HUANG Minglong and Friedel-Crafts acylation reaction in this study. The inhibitory effects of the new compounds were tested on NO production in LPS-induced mouse macrophage RAW264.7 cells, a cellular inflammation model. The structure-activity relationships were discussed. The structures of target compounds were confirmed by ESI-MS, 1H NMR and 13C NMR. In vitro activity experiments showed that 18 compounds had certain anti-inflammatory effects at the concentration of 40 μmol·L-1, of which 9a, 8b, 7c and 9c showed strong anti-inflammatory activities, and IC50 of 7c and 9c were comparable to the positive control drug ibuprofen.

     

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