共查询到16条相似文献,搜索用时 250 毫秒
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以布洛芬为原料,依次与草酰氯和氨基酸(2a~2d)反应制得中间体布洛芬衍生物(3a~3d);3与可缓慢释放H2S的5-对羟基苯基-1,2-二硫杂环戊烯-3-硫酮(4)经酯化反应,合成了4个新型的S-(+)-布洛芬衍生物(5a~5d)。α-溴乙酰氯与4经酯化反应制得5-(4-α-溴乙酰氧基)-苯基-1,2-二硫杂环戊烯-3-硫酮(6);6与1经偶联反应合成了一个新型的S-(+)-布洛芬衍生物(7),5和7的结构经1H NMR,IR和HR-MS表征。二甲苯致小鼠耳肿胀试验结果表明:5a,5c,5d和7均有较强的抗炎活性。 相似文献
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查尔酮及其衍生物是一类广泛存在于多种药物植物中的1,3-二苯基丙烯酮化合物,大多具有良好的生物活性。本文以2-噻吩甲醛和4-氟苯乙酮为原料,经3步反应,以较高收率合成了6个未见文献报道的哌嗪取代噻吩查尔酮衍生物(3a~3f),其结构经1H NMR, 13C NMR和HR-MS(ESI)表征。以地塞米松作阳性对照,采用细菌脂多糖诱导小鼠巨噬细胞Raw 264.7炎症模型对3a~3f的体外抗炎活性进行了初步测试。结果表明:化合物3d和3e能有效抑制炎症因子NO的生成(IC50分别为15.24 μM和19.05 μM)。 相似文献
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以萘普生(NPX)为前体,分别与芳基钌(Ru)、锇(Os)及铱(Ir)二聚体反应制备了3个单核配合物[Ru(η6-p-cymene)(NPX-bpy) Cl]Cl (1),[Os (η6-p-cymene)(NPX-bpy) Cl]Cl (2)和[Ir(η5-Cp*)·(NPX-bpy) Cl]Cl(3)。利用元素分析、电喷雾质谱和核磁共振波谱对3个配合物的组成和结构进行了表征,并研究了其细胞毒性。结果表明,3个配合物对几种肿瘤细胞株均无毒性(IC50>100μmol/L),仅配合物1对NB-4细胞有中等程度的毒性(IC50=45. 2μmol/L),且毒性大于配合物2和3,这可能与配合物1在细胞核内具有更高的富集量有关。此外,3个配合物均可有效抑制COX-2的表达,保留了萘普生的抗炎性质,实现了金属配合物抗癌及抗炎的多功能化应用。 相似文献
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去氢木香内酯是一种含有多种生物活性的倍半萜化合物,广泛存在于药材云木香中。去氢木香内酯与伯胺化合物经Michael加成反应,合成得到5个新的去氢木香内酯衍生物(1~5),其结构均经1H NMR、13C NMR和LC-MS确证。采用小鼠巨噬细胞Raw264.7模型初步测试了衍生物的抗炎活性和毒性,结果表明,化合物1对NO的生成抑制率为88±1.02%,表现出较好的抗炎活性,且在MTT实验中其对巨噬细胞的抑制率仅为3.75%,几乎无细胞毒性,可作进一步研究。 相似文献
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Chang Bin GUO Zhe Feng CAI Zong Ru GUO Zhi Qiang FENG Feng Ming CHU Gui-Fang CHENG 《中国化学快报》2006,17(3):325-328
Selective cyclooxygenase-2 (COX-2) inhibitors exhibite advantages for inflammation and pain relief without the gastrointestinal damage and hematologic liabilities observed with traditional non-steroidal anti-inflammatory drugs (NSAIDs) which can inhibit b… 相似文献
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Sulaiman Sulaiman Shabir Ahmad Syeda Sohaila Naz Sara Qaisar Sayyar Muhammad Amal Alotaibi Riaz Ullah 《Molecules (Basel, Switzerland)》2022,27(4)
Copper oxide nanoparticles (CuO NPs) were synthesized through the coprecipitation method and used as nanocarriers for etoricoxib (selective COX-2 inhibitor drug) and montelukast (leukotriene product inhibitor drug) in combination therapy. The CuO NPs, free drugs, and nanoformulations were investigated through UV/Vis spectroscopy, FTIR spectroscopy, XRD, SEM, and DLS. SEM imaging showed agglomerated nanorods of CuO NPs of about 87 nm size. The CE1, CE2, and CE6 nanoformulations were investigated through DLS, and their particle sizes were 271, 258, and 254 nm, respectively. The nanoformulations were evaluated through in vitro anti-inflammatory activity, in vivo anti-inflammatory activity, in vivo analgesic activity, in vivo anti-pyretic activity, and in vivo acute toxicity activity. In vivo activities were performed on albino mice. BSA denaturation was highly inhibited by CE1, CE2, and CE6 as compared to other nanoformulations in the in vitro anti-inflammatory activity. The in vivo bioactivities showed that low doses (5 mg/kg) of nanoformulations were more potent than high doses (10 and 20 mg/kg) of free drugs in the inhibition of pain, fever, and inflammation. Lastly, CE2 was more potent than that of other nanoformulations. 相似文献
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Herein, we review the recent progress in the synthesis of representative nonsteroidal anti-inflammatory drugs (NSAIDs), ibuprofen and naproxen. Although these drugs were discovered over 50 years ago, novel practical and asymmetric approaches are still being developed for their synthesis. In addition, this endeavor has enabled access to more potent and selective derivatives from the key frameworks of ibuprofen and naproxen. The development of a synthetic route to ibuprofen and naproxen over the last 10 years is summarized, including developing methodologies, finding novel synthetic routes, and applying continuous-flow chemistry. 相似文献