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1,3,4—噻二唑的α—氨基膦酸酯衍生物的合成及其生物活性 总被引:7,自引:4,他引:3
利用2-氨基-5-烷基-1,3,4-噻二唑、芳笛醛和亚磷酸三苯酯泊类Mannich反应,合成了一系列1,3,4-噻二唑的α-氨基膦酸酯生物。它们的结构级元素分析、IR,HNMR和MS这。初步生物活性测试结果表明,目标化合物对5种病人有一定的抑制作用。 相似文献
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1,2,3-噻二唑-4-乙酰胺(吗啉)类衍生物的合成与生物活性 总被引:1,自引:0,他引:1
以双乙烯酮为起始原料, 设计并合成了一系列新颖的1,2,3-噻二唑-4-乙酰苯胺(吗啉)类化合物, 通过元素分析、红外光谱、核磁共振氢谱和质谱对其结构进行了表征. 生物活性测试结果表明,部分化合物具有一定的抗TMV活性、 植物生长调节活性和杀菌活性. 相似文献
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以5-氨基-2-巯基-1,3,4-噻二唑为起始原料,对其2-位的巯基、5-位的氨基及杂环上3-位N原子进行结构修饰,合成了24个新型的1,3,4-噻二唑衍生物,其结构经1H NMR,13C NMR,IR和元素分析表征。 相似文献
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噻二唑及其衍生物的制备 总被引:14,自引:0,他引:14
合成了2,5-二流基-1,3,4-噻二唑及其八种胺盐衍生物和两种Mannich反应衍生物。测定了胺盐衍生物的部分物理常数和两种Mannich反应物的红外光谱、核磁1H谱数据,为杂环化合物润滑油添加剂的开发奠定基础。 相似文献
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噻二唑衍生物的合成及摩擦学性能研究 总被引:6,自引:0,他引:6
以 2 ,5-二巯基 -1 ,3,4 -噻二唑为原料合成了两种 2 ,5-二烷氧甲硫基 -1 ,3,4 -噻二唑衍生物 ,运用红外光谱′H核磁共振谱和元素分析测定了这些化合物的分子结构。在四球摩擦磨损试验机上考察了这两种化合物的极压、减摩和抗磨性能以及结构与性能的关系 ,并与ZDDP(T2 0 2 )进行了比较。结果表明 ,这些衍生物具有良好的极压和抗磨损性能 ,在低于 30 0N负荷条件下具有和T2 0 2 相似的抗磨损性能 ,而在高于 30 0N负荷和质量分数低于 1 %的条件下具有比T2 0 2 更好的抗磨损性能。 相似文献
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吡唑衍生物的合成及生物活性 总被引:15,自引:2,他引:15
以5-吡唑甲酰肼(7,8)为原料合成了4类共30种新化合物,这些化合物的结构均经^1H NMR,元素分析证实,部分化合物还经过了MS、IR确证,对大部分化合物做了生物活性测试,结果表明均具有一定的杀菌和除草活性。 相似文献
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以糠氯酸为原料,与叔丁基肼盐酸盐环合制得2-叔丁基-4,5-二氯-3(2H)哒嗪酮,随后与新合成的5-胺基-1,3,4-噻二唑-2-硫醇衍生物发生亲核取代反应,反应合成了11个新型1,3,4-噻二唑硫醚哒嗪酮衍生物(7a~7k)。化合物的结构均经1H NMR、13C NMR、IR、ESI-MS和元素分析表征。采用生长速率法测试了化合物对小麦赤霉病菌(G. zeae)、辣椒枯萎病菌(F. oxysporum)、苹果腐烂病菌(C. mandshurica)3种菌株的杀菌活性,在100 mg/L浓度下,化合物7a对小麦赤霉病菌的抑制率38.6%;7f对辣椒枯萎病菌的抑制率为54.6%。
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Xue-Ping Chu Qing-Fa Zhou Shen Zhao Fei-Fei Ge Mian Fu Jia-Peng Chen Tao Lu 《中国化学快报》2013,24(2):120-122
A group of 3-amino-2-pyrones were synthesized and their biological activities were evaluated for inhibiting cyclooxygenase(COX) activity.This study has led to the identification of COX-1-selective inhibitors.Among the tested compounds,the compound 5j exhibited the most potent COX-1 inhibitory activity(IC50 = 19.32μg/mL) and COX-1 selectivity index(SI = 41.98). 相似文献
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To find new lead compounds with high antifungal activity, a series of new thiourea derivatives containing 1,3,4-thiadiazole and thioether skeleton was designed via linking the active sub-structures. The target compounds were prepared via three steps from the commercially available thiosemicarbazide. Their structures were characterized by means of HRMS, 1H NMR, 13C NMR and IR spectroscopy. The preliminary results indicate that the title compounds show various antifungal activity against the tested fungi. Compounds 4c, 4g, 4h, 4k, 4n, 4o, 4p, 4q and 4r display excellent antifungal activities against one or more tested fungi with inhibitory efficiencies of 90%-100% at 200 μg/mL. Especially, compound 4o shows the best inhibitory effect against Curvularia lunata, Cotton Fusarium Wilt, P. P. var nicotianae and Fusarium spp. with the EC50 values of 28.12, 30.41, 15.2 and 6.22 μg/mL, respectively, which are even superior to those of triadimefon(98.73, 96.58, 105.37 and 102.18 μg/mL). The preliminary structure-activity relationship indicates that allyl and aromatic groups are favorable to their antifungal activities. 相似文献
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WANG Huan FU Yi-Feng FAN Zhi-Jin SONG Hai-Bin WU Qing-Jun ZHANG You-Jun Belskaya N. P Bakulev V. A. 《结构化学》2011,30(3):412-416
The title compound N-tert-butyl-N-(4-methyl-1,2,3-thiadiazole)-5-yl-N'-(4-me-thyl-1,2,3-thiadiazole)-5-formyl-N'-3,5-dichloropyrid-2-yl-diacylhydrazines (C18H17Cl2N7O3S2, Mr = 514.41) has been synthesized by the reaction of N-tert-butyl-N'-3,6-dichloropyridine-2-formyl hydrazine with 4-methyl-1,2,3-thiadiazole-5-carbonyl chloride and triethylamine, and its structure was characterized by 1H NMR, HR MS, and single-crystal X-ray diffraction. The crystal of the title compound belongs to monoclinic, space group C2/c with a = 27.726(8), b = 11.045(3), c = 14.507(4), β = 96.758(4)°, Z = 8, V = 4412(2) 3, Dc = 1.549 g/cm3, μ = 0.521 mm-1, F(000) = 2112, R = 0.0405 and wR = 0.1153. X-ray analysis indicates that all rings are non-planar in this molecule. The bioassay results indicate that both the title compound and the positive control RH-5992 have weak fungicide activities, while the title compound has good insecticidal activity against Plutella xylostella L. and no insecticidal activity against Culex pipiens pallens. 相似文献
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以2,5-二巯基-1,3,4-噻二唑为原料, 与水合肼缩合, 生成2,5-二肼基-1,3,4-噻二唑. 2,5-二肼基-1,3,4-噻二唑与苯甲酰氯反应生成2,5-二酰肼基-1,3,4-噻二唑, 以POCl3为环合剂环合酰肼基-1,3,4-噻二唑, 合成3,6-二取代苯基- 二-1,2,4-三唑并[3,4-b]-1,3,4-噻二唑衍生物, 合成的新化合物的结构通过元素分析、红外光谱、核磁共振氢谱和质谱予以证实, 并提出了环化反应机理. 相似文献
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合成了18个含有1H-1,2,4-三唑的咪唑[2,1-b]-1,3,4-噻二唑以及S-三唑[3,4-b]-1,3,4-噻二唑的稠杂环衍生物,经元素分析及谱学表征,探讨2,5,6-三取代咪唑[2,1-b]-1,3,4-噻二唑的可能生成机制.对大肠杆菌、绿脓杆菌、枯草杆菌等初步抑菌试验证明,多数化合物表现了较好的抑菌活性. 相似文献
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《Journal of Coordination Chemistry》2012,65(16-18):2814-2830
AbstractCo(II), Ni(II), and Cu(II) complexes of 2-Amino-5-ethyl-1,3,4-thiadiazole (AET) and 2-Amino-5-(ethylthio)-1,3,4-thiadiazole (AEST) have been synthesized and characterized based on elemental analysis, magnetic susceptibility, infrared (4000–400 cm?1), mass spectrometry (ESI and MALDI), UV–Vis (200–1100 nm) and thermal analysis (TGA/DTA). Molar conductance measurements proved that [M(L)2(H2O)2]Cl2·H2O are electrolytic complexes where M represents Co, Ni, and Cu divalent metal ions. The geometrical isomerism of [M(L)2(H2O)2]2+ ions were investigated by DFT-B3LYP calculations incorporated in Gaussian09 package; it favored the all trans isomers due to having the lowest energy points on the potential energy surface. The outcome of DFT-B3LYP quantum mechanical calculations using 6-31G(d) basis set favor six-coordinate sites via a bidentate ligand through exo amino and adjacent endo thiadiazole nitrogen (N3) donors. These results were consistent with magnetic measurements combined with infrared and UV–Vis spectral interpretations. The predicted metal–ligand binding energies from B3LYP/6-31G(d) calculations follow the trend Cu2+>Ni2+>Co2+, in agreement with the Irving–Williams series. Both AET and AEST ligands and the synthesized complexes were screened for their antibacterial activity and the outcome was high antimicrobial activity of the complexes compared to the free ligands against one or more microbial species and in some cases (copper complexes) higher activity than standard drugs. 相似文献