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A series of structurally novel 1,3,4-oxadiazole thioether derivatives(6a-6z) containing a 6-fluoroquinazolinylpiperidinyl moiety were designed and synthesized using pharmacophore hybrid approach,and their structures were fully characterized by ^1H NMR,13C NMR and HRMS spectra.Among them,the structure of compound 6 d was further corroborated via single-crystal X-ray diffraction analysis.In vitro antibacterial bioassays showed that compounds 6 a,6 g,6 u and 6 v possessed EC50 values of 30.4,30.6,27.5 and 26.0 μg/mL against phytopathogenic bacterium Xanthomonas oryzae pv.oryzae,respectively,which were significantly superior to that of commercially-available bactericide Bismerthiazol(85.1 μg/mL).Moreover,in vitro antifungal bioassays indicated that seven compounds demonstrated broad-spectrum fungicidal acitivties against six types of phytopathogenic fungi at 50 μg/mL.The present work showed the potential of 1,3,4-oxadiazole thioether derivatives carrying a 6-fluoroquinazolinylpiperidinyl moiety as effective antimicrobial agents for crop protection,deserving further investigations in the future. 相似文献
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《Arabian Journal of Chemistry》2023,16(2):104479
In the search for more efficient and versatile anti-phytopathogen agents, a series of new 1,3,4-oxadiazole thioether/sulfone analogues bearing a flexible N-containing heterocyclic pattern were elaborately prepared, and their bioactivities against plant pathogenic microorganisms were systematically evaluated. Bioassay screening results demonstrated that compounds 32 and 33 significantly inhibited the growth of Xanthomonas oryzae pv. oryzae (Xoo) in vitro (32, EC50 = 5.17 mg L?1; 33, EC50 = 1.19 mg L?1), which were significantly surpass commercial bismerthiazol (BT) and thiodiazole copper (TC). Meanwhile, pot experiments confirmed the prospective applications of compound 33 in managing rice bacterial leaf blight and its good safety toward rice plants. Further studies showed that compound 33 interfered with the formation of bacterial biofilms and inhibited bacterial virulence factors. Furthermore, an in vitro antifungal bioassay showed that compound 32 possessed remarkable growth inhibitory activity against Sclerotinia sclerotiorum (S.s., EC50 = 22.16 mg L?1) and Verticillium dahlia (V.d. EC50 = 32.78 mg L?1). These results all confirmed that the designed 1,3,4-oxadiazole compounds displayed potential for managing plant microbial diseases through targeting dihydrolipoamide S-succinyltransferase (DLST). 相似文献
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设计合成了18个以吡唑桥连1,3,4-噁二唑和1,3,5-三嗪的新型多杂环分子[7A(a~f),7B(a~f)和7C(a~f)];通过红外光谱(IR)、核磁共振波谱(NMR)和高分辨质谱(HRMS)等对目标分子进行了结构表征;评价了目标分子对蛋白酪氨酸磷酸酯酶1B(PTP1B)和细胞分裂周期25磷酸酯酶B(Cdc25B)的抑制活性.结果表明,所有目标分子对PTP1B和Cdc25B均有较好的抑制活性,其中,9个目标分子表现出优异的PTP1B和Cdc25B抑制效果,IC50值低于齐墩果酸(PTP1B抑制活性测试参照物)和正钒酸钠(Cdc25B抑制活性测试阳性参照物),有望成为潜在的PTP1B和Cdc25B抑制剂. 相似文献
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A new series of N^1-acetylamino-(5-alkyl/aryl- 1,3,4-thiadiazole-2-yl)-5-fluorouracil derivatives were designed and synthesized. These compounds have not been reported in literature, and their structure chemical were confirmed by IR, ^1H NMR and MS (HRMS). The results of antitumor inhibitory activity test showed that some compounds possess more potent antitumor inhibitory activity than 5-fluorouracil. 相似文献
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《Journal of Saudi Chemical Society》2014,18(3):255-261
In the present study, a novel series of 2-{5-[4-(1-aza-2-(2-thienyl)vinyl)phenyl](1,3,4-oxadiazol-2-ylthio)}-N-arylacetamides (IV)1–12 were synthesized and tested for their antimicrobial activity. Newly synthesized compounds were screened for their antibacterial and antifungal activities on Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, Staphylococcus pyogenes, Candida albicans, Aspergillus niger and Aspergillus clavatus. The chemical structures of newly synthesized compounds were elicited by IR, 1H NMR, 13C NMR and mass spectral data. The synthesized bio-active compounds exhibited excellent to moderate antimicrobial activity. Compounds (IV)5, (IV)6 and (IV)7 possess excellent antibacterial activity whereas compounds (IV)6, (IV)9 and (IV)11 possess excellent antifungal activity. 相似文献
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微波促进下2,5-二取代-1,3,4-(口恶)二唑衍生物的合成 总被引:9,自引:0,他引:9
报道了微波促进无溶剂条件下二酰基肼可以良好产率脱水闭环得到2,5-二取代-1,3,4-E二唑衍生物。反应产率受取代基影响较大,苯基取代时产率较高,烷基取代时产率较低;反应产率与所用的无机支持有关,其中以酸性三氧化二铝的效果最佳。此法不仅环境友好且操作安全,避免使用化学脱水剂。 相似文献
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In this work,the syntheses of new thermally stable poly(amide-imide)s with pendant 2-pyridyl-1,3,4-oxadiazole units in n-butyl methyl imidazolium bromide as reaction media have been reported.A new dicarboxylic acid has been derived from the reaction of diamine,2-(5-(3,5-diaminophenyl)-1,3,4-oxadiazole-2-yl)pyridine(POBD),and trimellitic acid anhydride.Polymers were prepared from the reaction of the diimide-diacid(DIDA) and different aromatic diamines in butyl methyl imidazolium bromide,[bmim][Br],in the ... 相似文献
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通过多亚甲基二溴化物桥连双合成了4个新配体合物,并通过元素分析,IR,UV和^1HNMR确定了它们的结构。 相似文献
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2-(4-Decarboxydehydroabietyl)-5-p-toyl-[1,3,4]-oxadiazole, C28H34N2O, has been synthesized and characterized by IR, NMR, elemental analysis and single-crystal X-ray diffraction method. The crystal belongs to the orthorhombic system, space group P212121 with a = 6.1351(5), b = 14.8495(19), c = 25.9050(2) A, V = 2360.0(4) A3, Z = 4, Mr = 414.57, Dc = 1.167 Mg/m^3, 2 = 0.71073 A,μ(MoKa) = 0.070 mm^-1, F(000) = 896, the final R = 0.0452 and wR = 0.1076 for 1647 observed reflections with I 〉 2σ(I). There are five rings in the crystal structure of the title compound, but the oxadiazole ring is non-coplanar with the benzene ring D. 相似文献
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Xu W He J He M Han F Chen X Pan Z Wang J Tong M 《Molecules (Basel, Switzerland)》2011,16(11):9129-9141
A series of new sulfone compounds containing 1,3,4-oxadiazole moieties were synthesized. The structures of these compounds were confirmed by spectroscopic data (IR, 1H- and 13C-NMR) and elemental analyses. Antifungal tests indicated that all the title compounds exhibited good antifungal activities against eight kinds of plant pathogenic fungi, and some showed superiority over the commercial fungicide hymexazol. Among them, compounds 5d, 5e, 5f, and 5i showed prominent activity against B. cinerea, with determined EC?? values of 5.21 μg/mL, 8.25 μg/mL, 8.03 μg/mL, and 21.00 μg/mL, respectively. The present work demonstrates that sulfone derivatives such as 5d containing a 1,3,4-oxadiazole moiety can be used as possible lead compounds for the development of potential agrochemicals. 相似文献
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Liangrun Dong Baojing Song Jian Wu Zengxue Wu Yunying Zhu Xuewen Chen 《Phosphorus, sulfur, and silicon and the related elements》2016,191(6):904-907
A series of novel thioether derivatives containing 1,3,4-oxadiazole/thiadiazole and emodin moieties were designed and synthesized. The structures of the target compounds were confirmed by 1H NMR, 13C NMR, Infrared, and elemental analysis. The results of bioactivity analysis showed that most of the target compounds exhibited moderate to good antiviral activity against tobacco mosaic virus at a concentration of 500 mg/L. Especially, among the title compounds, Y2, Y8, and Y10 possessed appreciable curative activity in vivo, with inhibition rates of 50.51, 52.08, and 54.62%, respectively, which were similar to that of Ningnanmycin (53.40%). 相似文献
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Jumat Salimon Nadia Salih Emad Yousif Ayad Hameed Ayad Kreem 《Arabian Journal of Chemistry》2010,3(4):205-210
In the present study a new acridone derivatives were synthesized. The newly synthesized compounds were characterized by IR, NMR and C, H, N, S analyses. All newly synthesized compounds were screened for their antibacterial (Staphylococcus aureus, Streptococcus viridans and Escherichia coil) and antifungal (Gibberela, Cercospora arachidicola, Physolospora piricola and Fusarium oxysporum) studies. The results revealed that all synthesized compounds have a significant biological activity against the tested microorganisms. 相似文献
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Zeba N. Siddiqui Farheen Farooq T.N. Mohammed Musthafa Anis Ahmad Asad U. Khan 《Journal of Saudi Chemical Society》2013,17(2):237-243
Two novel halopyrazole derivatives (3, 5) were synthesized from 5-chloro-3-methyl-1-phenylpyrazole-4-carboxaldehyde (1) using appropriate synthetic routes. Newly synthesized compounds were characterized using elemental analysis, spectral data (IR, 1H NMR, 13C NMR and mass spectrometry) and were evaluated for their in vitro antimicrobial activity. The minimum inhibitory concentration (MIC), minimum bactericidal concentration (MBC) and minimum fungicidal concentration (MFC) were determined for the test compounds as well as for reference standards. The investigation of antimicrobial screening revealed that compounds (3, 5) showed good antibacterial and antifungal activities, respectively. 相似文献
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De Qing LONG De Jiang LI Wei Quan CAI Sheng Sheng CHEN Department of Chemistry Yunyang Teachers College Hubei College of Chemical Engineering Wuhan University of Technology Wuhan 《中国化学快报》2006,(11)
Ten novel 2-alkylthio-5-(3, 4, 5-tribenzyloxyphenyl)-1, 3, 4-oxadiazole derivatives (5a-j) were synthesized from methyl 3, 4, 5-trihydroxybenzoate by etherification, hydrazidation, cyclization and thioetherification reactions. The structures of 5a-j were confirmed by 1HNMR, MS spectra and elemental analysis. The results indicated that most of the compounds 5 exhibited good fungicidal activities. The activity of 5h is higher than 90% against Fusarium oxysporum and Botrytis cinereapers in 50 mg/L. 相似文献