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Zai-Gang Luo Yu Zhao Chao Ma Xue-Mei Xu Xiao-Mei Zhang Nian-Yu Huang Hong-Qiu He 《中国化学快报》2014,25(5):737-740
A series of novel calix[4]arene derivatives incorporating two triazolyl 1 3-diketo subunits in alternate positions at the lower rim were synthesized and screened for HⅣ integrase inhibition activity.The chemical structures of these compounds were confirmed by means of1H NMR 13C NMR,and ESI-MS.Preliminary bioassays indicated that calix[4]arene derivatives proved to be more active than p-tertbutylcalix[4]arene derivatives.In particular,compound 4g presented the most potent integrase strand transfer inhibitory activity with an IC50value of 6.1 mmol/L. 相似文献
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TANG Xiaobin LI Zhenghui LI Yonghong LIU Wei YU Peng LI Lixin GUO Yu YANG Cheng 《高等学校化学研究》2015,31(1):71-77
A series of novel saccharin derivatives containing 1,2,3-triazole moiety was synthesized in satisfactory yields. The structures of all the compounds were elucidated and confirmed by Fourier transform infrared(FTIR) spectroscopy, 1H and 13C nuclear magnetic resonance(1H NMR, 13C NMR) spectroscopy, and high resolution mass spectrometry(HRMS). The bioassays indicated that most of the title compounds displayed some extent herbicidal activities at 100 μg/mL. 相似文献
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A series of novel 1-glycosyl-4-{N-[(2'-morpholinethoxy)phenyl]aminomethyl}-1H-1,2,3-triazoles was designed and synthesized through a simple and efficient multistep synthetic method in good yields. The 1,2,3-triazole moiety acted as a single disubstituted ring and a linker between carbohydrates(D-glucose, D-galactose, maltose and lactose) and morpholine. The compounds were characterized by 1H NMR, 13C NMR and mass spectra(MS). Two different deprotection methods were discussed. The effects of compounds 5a, 5c and 6e on the intracellular calcium ion concentration([Ca2+]i) in the central neurons of S. exigua were well investigated by calcium imaging technique. The results demonstrated that compound 6e could elevate the calcium concentration in the glial cells, not in the neurons. 相似文献
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LI Jing LIU Hongwei MENG Fanyu YAN Liuqing SHI Yanpeng ZHANG Yumin GU Qiang 《高等学校化学研究》2018,34(2):197-202
A comparison synthesis of 1,2,3-triazoles bearing isoxazole ether was developed between conventional and microwave-assisted heating. Single/double 1,2,3-triazoles bearing isoxazole ether were synthesized by click reaction starting from substituted isoxazolyl alkyne compounds and substituted benzyl azide compounds or neopentylglycol diazide in the presence of copper(I) that in-situ generated. Herein, the effect of different catalysts on the yield was researched by conventional method, and the optimal catalyst was selected. The structures of all the synthesized compounds were confirmed by MS, FTIR, 1H and 13C NMR spectroscopies. Moreover, the crystal structure of 5-{[(1-benzyl-1H-1,2,3-triazol-4-yl)methoxy]methyl}-3-(4-fluorophenyl)isoxazole(2h) was determined. 相似文献
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邻甲氧基羰基苄氧基取代杯[4]芳烃衍生物的合成及其性能研究 总被引:1,自引:0,他引:1
杯芳烃是继冠醚、环糊精之后的第三代主体分子[1].据文献[2,3]报道,在杯[4]芳烃下沿酚氧原子上连接乙酸酯得到的四取代衍生物对Na+有很高的选择性,核磁与晶体结构研究均证实这是由于羧酸酯的羰基和酚氧基参与了对Na+的配位,而且配位基团所形成的包络空间大小与钠离子相匹配.一般认为,随着包络空间改变,对金属离子的识别作用会有所变化[4].但目前对这方面的工作并没有给予更多的重视.我们发现,用2-溴甲基苯甲酸甲酯与杯[4]芳烃反应,得到了一种新的四取代杯[4]芳烃衍生物[2]萃取研究结果表明,该化合物对钾离子有较好的选择性.此外,在合成该衍生物的过程中,还得到了另一新的二取代衍生物(3). 相似文献
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以1,2,4-三唑为核心结构的杂环分子,因其优良而广泛的生物活性,已成为药物筛选中重要的研究对象。 本文为了研究其构效关系,针对1,2,4-三唑结构中3个位点分别进行不同的结构修饰,并将其与哌嗪和均三嗪分别偶联,首次合成了两类共28个双三唑多杂环目标分子[TM1TM3(af)]和[TM4TM5(ae)]。 为了比较三唑中4-氨基对生物活性的影响,还与化合物6-吗啉-2,4-(5-硫醚基-4-氨基-3-正戊基1,2,4-三唑)-1,3,5-三嗪(C)和6-吡咯-2,4-(5-巯基-4-氨基-3-正戊基-1,2,4-三唑)-1,3,5-三嗪(D)进行了比较。 通过傅里叶变换红外光谱仪(IR)、核磁共振谱(1H NMR)和高分辨率质谱仪(HRMS)等技术手段对28个目标分子进行了结构表征,研究了其对细胞分裂周期25磷酸酯酶B(Cdc25B)的抑制活性。 结果表明,21个目标分子表现出优良的抑制活性,9个目标分子的抑制活性优于阳性参照物,有望成为抗肿瘤药物先导物。 相似文献
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使用相应的w-硫醚羧酸酰氯与杯[4]芳烃或者偶氮杯[4]芳烃酰化合成了一类新型的杯[4]芳烃衍生物。分离得到六个新化合物4a-4c和5a-5c,并使用MALDI, EA, 1H和13C NMR进行了表征。NMR图谱表明偶氮杯[4]芳烃衍生物 5a-5c均为1,3-转换构型,而4a-4c则均为锥式构型。对偶氮杯[4]芳烃衍生物5a-5c的红外和紫外性质也进行了研究。 相似文献
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MAO Ming-zhen LI Yu-xin ZHOU Yun-yun YANG Xiao-ping ZHANG Xiu-lan ZHANG Xiao LI Zheng-ming 《高等学校化学研究》2013,29(5):900-905
A series of novel 1-substituted phenyl or glycosyl 1,2,3-triazoles was designed and synthesized by azide-alkyne 1,3-dipolar cycloaddition between 4,6-dimethoxy-2-[(4-prop-2-ynyl)piperazin-1-yl]pyrimidine and each of different azides catalysed by in situ generated Cu(I). The O-acyl protecting groups on glycosyl 1,2,3-triazoles were removed by triethylamine in wet methanol. Their chemical structures were established on the basis of corresponding 1H NMR, 13C NMR, MS and elemental analysis. The fungicidal activities of target compounds were evaluated in vitro against Fusarium omysporum, Physalospora piricola, Alternaria solani, Phytophthora capsici, Cercospora arachidicola and Gibberella zeae at 50 μg/mL. The bioassay results indicate that some of the compounds exhibited mode-rate but promising fungicidal activities. In particular, acetylated glucopyranosyl triazole displayed a good fungicidal activity against Physalospora piricola, which is equal to that of the positive control compound chlorothalonil. 相似文献
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以间苯二酚为原料,经5步反应制得中间体4,4′-[4,6-双(己氧基)-1,3亚苯基]双{1-[4-(叠氮甲基)苯基]-1H-1,2,3-三氮唑}(6); 6与1,5-二乙炔基-1,4-二(己氧基)苯在高度稀释的条件下经Click反应环合制得1,2,3-三唑环蕃(7); 7与三甲基氧鎓四氟硼酸盐反应合成了全甲基化的新型1,2,3-三唑鎓环蕃,其结构经1H NMR, 13C NMR和HR-ESI-MS表征。 相似文献
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《Mendeleev Communications》2022,32(1):103-104
Novel first-generation dendrimers on the calix[4]resorcinol core with four branches each containing multiple 1,2,3-triazole units have been synthesized in one-step by acid catalyzed condensation of resorcinols with a new aldehyde dendron, namely, 4-{3,5-bis[(1-benzyl-1H-1,2,3-triazol-4-yl)- methoxy]benzyloxy}benzaldehyde (obtained by alkyne–azide cycloaddition). The reaction proceeds stereoselectively to form rccc-diastereoisomers in high yields. 相似文献
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The artificial receptors with multiple recognition site had been synthesized by linking two unsymmetrical monofunctionalized porphyrin to p-tert-butyl calix[6]-arene via two flexible chain, followed by inserting metal ion into the porphyrin species.The structures (see Fig 1) of these calix[6]arene-diporphyrins and their metal complexes were confirmed by UV-vis spectra, IR spectra, mass spectra, 1NMR spectra(600 MHz) and/or 13C NMR. Their conformations were investigated preliminarily by UV-vis spectra and computer simulation. In constrast with the correspounding porphyrin monomer, the soret bond of calix[6]arene-diporphyrins in UV-vis spectra showed hypsochromic shift. This phenomenon suggested that two porphyrin rings maintain a face to face parallel conformation, as confirmed by computer simulation that showed the conformation energy is the lowest as two porphyrin rings hold such a conformation. Besides, simplicity of the 1NMR spectra indicates that the conformation of calix[6]arene-diporphyrin possesses high symmetry. Therefore,the calix[6]arene must be cone conformation. 相似文献
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Jing-Peng Zhang Xiang-Yang Li Ya-Wen Dong Yao-Guo Qin Xin-Lu Li Bao-An Song Xin-Ling Yang 《中国化学快报》2017,28(6):1238-1242
To find new lead compounds with high biological activity,a series of novel 4-methyl-1,2,3-thiadiazole-5-carboxaldehyde benzoyl hydrazone derivatives were designed and synthesized.Their structures were confirmed by ~1H NMR,~(13)C NMR,IR spectrum and elemental analysis.Preliminary bioassay indicated that the title compounds exhibited moderate to strong fungicidal activity against six fungi in vitro at50 μg/mL.Moreover,some of the title compounds exhibited good curative activity against TMV in vivo at500 μg/mL.The structure-activity relationship analysis of compounds against Valsa mali showed that compounds containing halogen at the para position on phenyl exhibited the best activity.Especially compound 8k showed broad spectrum fungicidal activities against Valsa mali,Botrytis cinerea,Pythium aphamdermatum,Rhizoctonia solani,Fusarium moniliforme and Altemaria solani with the EC_(50) values of8.20,24.42,15.80,40.53,41.48,and 34.16 μg/mL,respectively. 相似文献
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Synthesis and Crystal Structure of 3,6-Bis(4-methyl-1,2,3-thiadiazol-5-yl)-1,2,4-triazolo[3,4-b][1,3,4]thiadiazole 总被引:1,自引:0,他引:1
The compound 3,6-bis(4-methyl-1,2,3-thiadiazol-5-yl)-1,2,4-triazolo[3,4-b][1,3,4] thiadiazole(C9H6N8S3,Mr = 322.40) has been synthesized by the reaction of 4-amino-3-(4-methyl-1,2,3-thiadiazolyl)-5-mercapto-1,2,4-triazole with 4-methyl-1,2,3-thiadiazol-5-carboxylic acid and phosphorus oxychloride,and its structure was characterized by IR,1H NMR,EI-MS,elemental analysis and single-crystal X-ray diffraction.The crystal of the title compound belongs to monoclinic,space group C2/c with a = 2.0053(4),b = 1.3081(3),c = 1.0556(2) nm,β = 112.69(3)°,Z = 4,V = 2.5548(9) nm3,Dc = 1.676 g/cm3,μ = 0.582 mm-1,F(000) = 1312,R = 0.0546 and wR = 0.1523.X-ray analysis indicates that all rings are essentially planar in this molecule,and an intermolecular hydrogen bond C(9)-H(9)…N(2) and weak intramolecular interactions between S(1)…N(7),S(3)…N(1) and S(2)…N(4) are observed. 相似文献
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A series of novel tetrahydroimidazo[1,2-a]pyridine-5(1H)-one derivatives containing a electronegative pharmacophore(=CNO2) were synthesized via practical aza-ene reaction and characterized by 1H NMR, 13C NMR, 19F NMR and HRMS. Preliminary bioassays showed that some of the target compounds exhibited good insecticidal activity against brown planthopper(Nilaparvata lugens) and cowpea aphids(Aphis craccivora) at 500 mg L-1. Among them, compound 11h was active against brown planthopper at 100 mg L-1. The insecticidal activities varied significantly depending on the types and patterns of the substituents, which provided guidance for further investigation on structure modifications. 相似文献
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Irina R. Knyazeva Karina M. Mukhamedyanova Victor V. Syakaev Aidar T. Gubaidullin Wolf D. Habicher Alexander R. Burilov 《Tetrahedron letters》2018,59(17):1683-1685
Novel calix[4]resorcinols containing four triazole fragments on the aromatic substituents of the calixarene framework were synthesized via a one-step condensation of resorcinol and its derivatives with 4-(1-benzyl-1H-[1,2,3]triazol-4-ylmethoxy)benzaldehyde. The macrocyclic products are rctt- and/or rccc-isomers, which were isolated and characterized by NMR and single crystal X-ray diffraction studies. The same products were also prepared via the click-reaction of benzyl azide with previously synthesized calix[4]resorcinols containing four alkyne terminal groups on the aromatic substituents. In this case, only rctt-diastereomers of the corresponding calixarenes were isolated, which is governed by conformational features of the starting macrocycles. 相似文献
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Antal Csmpai Pter Kvr Gyrgy Hajs Zsuzsanna Riedl 《Journal of Molecular Structure》2002,616(1-3):73-78
Alkylation of some selected [1,2,3]triazolo[4,5-d]pyridazines having five or more nitrogen atoms capable for alkylation was investigated. Pyridyl derivatives substituted also on the [1,2,3]triazole ring gave quaternary pyridinium salts, whereas in the case of the analogues compounds unsubstituted at the triazole moiety, the alkylation of the triazole ring was also observed. Unambiguous structure elucidation was provided by 1H–15N HMBC experiments which also allowed the assignment of the 15N NMR shifts. 相似文献