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为改善二唑及三唑类化合物的生物活性, 设计合成了一系列多氟烷基乙基取代的1,3,4-噁二唑-2-硫酮6a~6l及1,2,4-三唑-5-硫酮类化合物9a~9l. 1H NMR, 19F NMR, IR和MS谱以及元素分析表征了它们的结构; 实验结果与Materials Studio 3.0中的Dmol3计算模块理论计算表明了唑环上的NH较之CONH中的NH更易进行烷基化反应. 相似文献
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N-芳基-N'-[(4-吡啶基)羰基]氨基硫脲用85%的水合肼环化, 得到3-(4-吡啶基)-4-氨基-5-芳氨基-1,2,4-三唑(2a~2c). 然后再与3-甲酰基色酮(3a~3d)反应, 制备得到了一系列新化合物: 3-(4-吡啶基)-4-(6-取代色酮-3-基亚甲氨基)-5-芳氨基-1,2,4-三唑(4a~4c, 5a~5c, 6a~6c, 7a~7c). 化合物的结构经元素分析, IR, 1H NMR和MS确证. 相似文献
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以取代苯和丁二酸酐为起始原料, 经Friedel-Crafts反应, 肼合环, Br2/HOAc氧化脱氢后得到一系列1,6-二氢-3-芳基-6-哒嗪酮(2a~2d). 然后将2a~2d与PCl5在POCl3中回流, 得到相应的氯代产物3a~3d, 将其与酰肼作用, 合环后得到一系列未见报道的哒嗪并[3,2-c]1,2,4-三唑类化合物. 所有化合物结构均经元素分析, IR, 1H NMR 和MS谱得以证实, 并对其波谱性质进行了讨论. 相似文献
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N-芳基-2-[(吡啶-4-基)羰基]氨基硫脲1a~1e用NaOH溶液环合, 得到3-巯基-4-芳基-5-(吡啶-4-基)-1,2,4-三唑(2a~2e), 经酯化, 肼解, 得S-{[4-芳基-5-(吡啶-4-基)]-1,2,4-三唑-3-基}巯乙酰肼(3a~3e), 再与3-甲酰基色酮(4a~4d)反应, 合成得到了一系列新化合物5a~5e, 6a~6e, 7a~7e, 8a~8e. 化合物的结构经元素分析, IR, 1H NMR和MS谱确证. 相似文献
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N-多氟烷基取代和葡萄糖基取代的1,2,4-三唑-5-硫酮类席夫碱的合成及其杀虫活性 总被引:3,自引:0,他引:3
为改善三唑类化合物的生物活性, 以3-苯基-4-氨基-1,2,4-三唑-5-硫酮为原料, 将其与芳香醛在冰醋酸体系中反应, 得到3-苯基-4-芳基亚甲氨基-1,2,4-三唑-5-硫酮类席夫碱(4a~4i). 在此基础上, 化合物4a~4i分别与多氟烷基碘代烷和溴代乙酰基葡萄糖反应合成了一系列1,2,4-三唑-5-硫酮类席夫碱的多氟烷基取代物5a~5r和葡萄糖基取代物6a~6d, 并用1H NMR, 19F NMR, IR和MS谱以及元素分析表征了它们的结构. 初步生物活性测试结果表明, 部分目标化合物具有明显的杀虫活性. 相似文献
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采用微波和相转移催化法通过1-苯基-5-(4-苯基-1,2,4-三唑-5-巯基-3-甲硫基)四唑(2)与2-氯乙酰芳胺(3)反应高效、快速地合成了10种尚未见文献报道的1-苯基-5-[5-(芳胺羰基甲硫基)-4-苯基-1,2,4-三唑-3-甲硫基]四唑. 其结构经 IR, 1H NMR, 13C NMR 和元素分析表征. 生物活性实验结果表明, 该类化合物在较低浓度下部分化合物对小麦芽有很好的促进作用. 相似文献
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型2,3-二氢-3-芳亚甲基-4-芳基-1,5-苯并硫氮杂的合成及表征 总被引:1,自引:1,他引:0
在盐酸和乙醇存在下, 苯乙酮、多聚甲醛以及N,N-二甲基甲酰胺进行Mannich反应, 得到了Mannich碱; 将其和1,2,4-三唑在水中反应, 得到含有1,2,4-三唑的苯丙酮; 然后, 在哌啶和甲苯存在下, 苯丙酮和苯甲醛进行羟醛缩合, 得到一系列含有1,2,4-三氮唑的查尔酮; 最后, 在三氟乙酸的催化下, 查尔酮和邻氨基硫酚发生亲核取代反应, 然后脱水缩合, 合成了一系列2,3-二氢-3-芳亚甲基-4-芳基-1,5-苯并硫氮杂. 其结构经IR, 1H NMR, MS及元素分析确证. 相似文献
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以α-氨基乙酸和芳基异硫氰酸酯为起始原料制备3-芳基-2-硫乙内酰脲, 然后在酸性条件下与3-甲酰基色酮发生类Knoevenagel缩合反应, 合成得到了16种新的5-(色酮-3-亚甲基)-3-芳基硫乙内酰脲类化合物. 所有化合物的结构均经IR, 1H NMR, LC-MS和元素分析确证, 并做了初步的生理活性测试 相似文献
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铌取代型钨硅杂多酸盐的合成及抗病毒活性研究 总被引:14,自引:4,他引:10
杂多化合物因具有独特的结构和优异的抗病毒活性[1,2],近年来受到普遍重视,但研究的热点主要集中在抗艾滋病毒(HIV)、疱疹病毒(HSV)、抗肿瘤等方面[3,4],而忽视了对植物病毒防治的研究。 相似文献
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《Macromolecular bioscience》2018,18(2)
Stem cells are a promising cell source for regenerative medicine due to their differentiation and self‐renewal capacities. In the field of regenerative medicine and tissue engineering, a variety of biomedical technologies have been tested to improve proangiogenic activities of stem cells. However, their therapeutic effect is found to be limited in the clinic because of cell loss, senescence, and insufficient therapeutic activities. To address this type of issue, advanced techniques for biomaterial synthesis and fabrication have been approached to mimic proangiogenic microenvironment and to direct proangiogenic activities. This review highlights the types of polymers and design strategies that have been studied to promote proangiogenic activities of stem cells. In particular, scaffolds, hydrogels, and surface topographies, as well as insight into their underlying mechanisms to improve proangiogenic activities are the focuses. The strategy to promote angiogenic activities of hMSCs by controlling substrate repellency is introduced, and the future direction is proposed. 相似文献
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Eight Schiff bases have been synthesized using 3‐alkyl‐4‐amino‐1,2,4‐triazole‐5‐thione and substituted benzaldehyde as starting materials. The structures of the compounds have been confirmed by 1H NMR, IR and elemental analysis and their biological activities to five vegetable pathogens have been tested. The results showed that they exhibited good fungicidal activities. 相似文献
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A series of 4-arylidenamino-5-phenyl-4H-1,2,4-triazole-3-thiols have been synthesised and their inclusion complexes have been prepared with β-cyclodextrin. The compounds and their inclusion complexes have been characterised by studying their physical and spectral properties. The thermodynamic stability constant and free energy of activation have been determined to know the stability of inclusion complexes. Finally, the compounds and their inclusion complexes are screened for antibacterial, antioxidant and anthelmintic activities. It is found that inclusion complexes of the newly synthesised compounds have appreciable stability and inclusion complex formation increases the antibacterial, antioxidant and anthelmintic activities significantly as compared to naked compound. 相似文献
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Mancini I Sicurelli A Guella G Turk T Macek P Sepcić K 《Organic & biomolecular chemistry》2004,2(9):1368-1375
Dimers and tetramers of linear 3-alkylpyridinium salts have been synthesized by an efficient synthetic pathway, which is also applicable to the preparation of higher oligomers. Mono-, di- and tetrameric compounds have been tested for antibacterial and hemolytic activities and for the inhibition of acetylcholinesterase and protein phosphatase 2A. Their activities were compared to those of the natural poly-3-octylpyridinium alkaloids isolated from the Mediterranean sponge Reniera sarai. Relatively high antibacterial and anti-acetylcholinesterase activities were observed that increase with higher degrees of oligomerization. 相似文献
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1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮与对氨基苯乙酮的缩合反应、量化计算和抑菌活性 总被引:3,自引:0,他引:3
利用1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮(PMBP)和对氨基苯乙酮(PAAP)制备了PMBP缩对氨基苯乙酮(PMBP缩PAAP)及其铜(Ⅱ)、钴(Ⅱ)、镍(Ⅱ)和锌(Ⅱ)配合物,根据元素分析、红外、紫外、MS和1H NMR谱表征了结构.利用量子化学和分子力学计算方法对缩合反应的机理进行了探讨,较好地解释了PMBP-PAAP配体的烯胺酮式构型及其配合物的亚胺烯醇式构型.测定了化合物对大肠杆菌和金黄色葡萄球菌的抑制活性,其中以钴(Ⅱ)和铜配合物(Ⅱ)的抑菌活性最佳. 相似文献
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The crystal structures of different forms of TiO2 and those of BaTiO3, ZnO, SnO2, WO3, CuO, Fe2O3, Fe3O4, ZrO2 and Al2O3 nanoparticles have been deduced by powder X-ray diffraction. Their optical edges have been obtained by UV-visible diffuse reflectance spectra. The photocatalytic activities of these oxides and also those of SiO2 and SiO2 porous to oxidize iodide ion have been determined and compared. The relationships between the photocatalytic activities of the studied oxides and the illumination time, wavelength of illumination, concentration of iodide ion, airflow rate, photon flux, pH, etc., have been obtained. Use of acetonitrile as medium favors the photogeneration of iodine. 相似文献
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"色谱行业女学者联谊会"自2016年4月成立以来,共举行学术交流和技术交流活动14次,相关报告28人次,参会人员600余人次。与《色谱》期刊合作,2017年3月首次出版了"庆祝国际劳动妇女节色谱行业女学者专刊",发表论文22篇;2018年3月,该专刊发表论文20篇。联谊会还建立了女学者微信群,女学者联谊会活动通过微信实时报道14次。联谊会活动受到色谱行业广大学者和同行的关注。在联谊会成立两周年之际,我们回顾联谊会的活动,借此感谢所有女学者的积极参与,感谢色谱行业各方同仁的支持与帮助。 相似文献