Novel 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones and cyclohexanols as analgesic and anti-inflammatory agents

Dan Liu; Weishe Yu; Jingjing Li; Cong Pang; Linxiang Zhao

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Novel 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones and cyclohexanols as analgesic and anti-inflammatory agents

机译：新型2-（E）-取代的亚苄基-6-（N-取代的氨基甲基）环己酮和环己醇作为镇痛药和消炎药

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Twenty-two new 2-(E)-substituted benzyli-dene-6-(N-substituted aminomethyl)cyclohexanones (6a-6j) and cyclohexanols (7a-71) were designed and synthesized. Target compounds were obtained through Stork enamine, Mannich, and Grignard reactions taking cyclohexanone as starting material. The structures were confirmed by the application of IR, ~1H NMR, MS, and HR-MS data. The analgesic activities were evaluated by acetic acid-induced writhing test and hot plate method. The anti-inflammatory activities were assayed by xylene-induced ear swelling and carrageenan-induced paw edema in mice model. All tested compounds showed analgesic and anti-inflammatory capacities in oral administration. Some compounds (6a, 6c, 6h, 6i, 7c, 7h, and 7i) displayed the moderate analgesic activity compared with positive control ibuprofen, and some compounds (6a, 6b, 6d, 6h, 7a, and 7d) exhibited more anti-inflammatory activity than ibuprofen. Among them, compound 6a could be a potential nonsteroidal anti-inflammatory agent with significant analgesic activities and remarkable anti-inflammatory activities. Further research is being conducted.

机译：设计并合成了二十二种新的2-（E）-取代的苄基-二烯-6-（N-取代的氨基甲基）环己酮（6a-6j）和环己醇（7a-71）。通过以环己酮为起始原料的Stork enamine，Mannich和Grignard反应获得目标化合物。通过应用IR，〜1H NMR，MS和HR-MS数据确认了结构。通过乙酸诱导的扭体试验和热板法评价其镇痛活性。通过二甲苯诱导的小鼠耳朵肿胀和角叉菜胶引起的爪水肿来测定抗炎活性。所有测试的化合物在口服给药中均显示出镇痛和抗炎的能力。与阳性对照布洛芬相比，某些化合物（6a，6c，6h，6i，7c，7h和7i）显示出中等的镇痛活性，而某些化合物（6a，6b，6d，6h，7a和7d）则显示出更多的抗炎症活性比布洛芬高。其中，化合物6a可能是潜在的非甾体类抗炎药，具有显着的止痛活性和显着的抗炎活性。正在进行进一步的研究。

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来源
《Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents》 |2013年第8期|共8页
作者
Dan Liu; Weishe Yu; Jingjing Li; Cong Pang; Linxiang Zhao;
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正文语种 eng
中图分类药学;
关键词
2-(E)-Substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones; 2-(E)-Substituted benzylidene-6-(N-substituted aminomethyl)-l-aryl-cyclohexanols; Analgesia; Anti-inflammation;

机译：2-（E）-取代的亚苄基-6-（N-取代的氨基甲基）环己酮;2-（E）-取代的亚苄基-6-（N-取代的氨基甲基）-1-芳基-环己醇;镇痛;消炎;

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1. Novel 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones and cyclohexanols as analgesic and anti-inflammatory agents [J] . Dan Liu, Weishe Yu, Jingjing Li, Medicinal chemistry research: an international journal for rapid communications on design and mechanisms of action of biologically active agents . 2013,第8期

机译：新型2-（E）-取代的亚苄基-6-（N-取代的氨基甲基）环己酮和环己醇作为镇痛药和消炎药
2. Novel 2-(nitrooxy)ethyl 2-(4-(substituted phenyl)-2-((substituted phenyl)amino)thiazol-5-yl)acetate as Anti-inflammatory, Analgesic and Nitric Oxide Releasing Agents: Synthesis and Molecular Docking Studies [J] . Aniket P. Sarkate, Deepak K. Lokwani, Kshipra S. Karnik, Anti-Inflammatory & Anti-allergy Agents in Medicinal Chemistry . 2017,第3期

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Novel 2-(E)-substituted benzylidene-6-(N-substituted aminomethyl)cyclohexanones and cyclohexanols as analgesic and anti-inflammatory agents

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