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哒嗪酮

哒嗪酮的相关文献在1986年到2022年内共计437篇,主要集中在化学、化学工业、药学 等领域,其中期刊论文85篇、会议论文10篇、专利文献52049篇;相关期刊42种,包括药学实践杂志、药学学报、中国药物化学杂志等; 相关会议9种,包括中国化学会第三届全国分子手性学术研讨会、第八届全国新农药创制学术交流会、中国化工学会农药专业委员会第十二届年会等;哒嗪酮的相关文献由1007位作者贡献,包括邓莉平、王玮、A·布劳卡特等。

哒嗪酮—发文量

期刊论文>

论文:85 占比:0.16%

会议论文>

论文:10 占比:0.02%

专利文献>

论文:52049 占比:99.82%

总计:52144篇

哒嗪酮—发文趋势图

哒嗪酮

-研究学者

  • 邓莉平
  • 王玮
  • A·布劳卡特
  • D·多施
  • O·沙特
  • F·施蒂贝尔
  • 河村保夫
  • 席眉扬
  • 小仓友幸
  • T·M·史蒂文森
  • 期刊论文
  • 会议论文
  • 专利文献

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    • 胡伟男; 朱梅; 漆亚云; 陈洁; 唐思雨; 唐震华; 王贞超; 欧阳贵平
    • 摘要: 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、MS(ESI)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%.
    • 石延霞; 张晓慧; 谢学文; 柴阿丽; 徐玉芳; 赵振江; 李宝聚
    • 摘要: 吡唑并嘧啶衍生物((E)-N-(2-氟-4-三氟甲基苯乙烯基)-1-甲基-1H-吡唑并[3,4-d]嘧啶-4-胺,简称BDO-1)和哒嗪酮衍生物(4-羟基-1-(4-甲氧基苯基)-6-氧代-1,6-二氢吡嗪-3-甲酸甲酯,简称PDZ-1)是由华东理工大学创制并合成的新化合物,本研究分别测定了其离体抑菌活性及其诱导抗病活性,并对田间应用技术进行了研究。结果表明:离体抑菌试验结果显示,BDO-1和PDZ-1对供试黄瓜的尖孢镰孢菌和多主棒孢菌并无杀菌活性;温室盆栽试验发现,2个化合物对7种蔬菜病害具有明显的诱导抗病活性,其中:BDO-1在10 mg/L下对黄瓜细菌性角斑病、黄瓜棒孢叶斑病、黄瓜枯萎病、黄瓜霜霉病、番茄早疫病、番茄灰叶斑和辣椒疫病的防治效果分别为58.81%、61.79%、69.88%、64.14%,54.42%、54.85%和63.59%;PDZ-1在10 mg/L下对黄瓜细菌性角斑病和黄瓜棒孢叶斑病的防治效果分别为62.33%和59.15%。田间防治效果验证结果表明,BDO-1和PDZ-1对黄瓜枯萎病的防治效果分别为62.95%和48.45%。研究发现,BDO-1和PDZ-1在质量浓度为10 mg/L、诱导5次、每次间隔5d的条件下施用,对黄瓜枯萎病和棒孢叶斑病可发挥最佳防治效果。
    • 王道宇; 牟甜甜; 赵祚全; 郭风; 张现忠; 方纬
    • 摘要: 目的:通过初步动物实验,评价4-氯-2-叔丁基-5-[[6-[[4-(2-氟-18F-乙基)-1H-1,2,3-三唑-1-基]甲基]-2-吡啶基]甲氧基]-3(2H)-哒嗪酮(18F-FPTP2)用于心肌灌注发射型正电子断层显像(PET)的可能性。方法:采用18F-F-取代OTs前体的方法进行标记,通过HPLC非梯度洗脱进行纯化,并通过HPLC确认标记化合物结构。中华小型猪经静脉注射18F-FPTP2(37 MBq/15 kg),并于注射后2 min、10 min、20 min、30 min、40 min、50 min和60 min分别进行PET/CT扫描。结果:18F-FPTP2制备的总时间为70 min,未校正的放化产率为(25±7.2)%,放射化学纯度>98%。PET研究表明,18F-FPTP2在中华小型猪中的心肌摄取随时间的延长而增加,靶器官与非靶器官比值亦随之增加。注射后2 min,心和(或)肝以及心和(或)肺放射性摄取比值分别为0.65±0.10和3.47±0.29。注射后60 min,心和(或)肝以及心和(或)肺放射性摄取比值分别为0.92±0.13和9.28±0.77。结论:18F-FPTP2能够被心肌组织摄取而显影清晰,但心和(或)肝放射性摄取比值需要进一步提高。%Objective: To preliminarily evaluate the potential of 2-tert-butyl-4-chloro-5-((6-((4-(2-[18F]fluroethyl)-1H-1,2,3-triazol-1-yl)methyl)-2-pyridinyl)methoxy)-3(2H)-pyridazinone ([18F]FPTP2) as a myocardial perfusion imaging agent, by animal positron emission tomography(PET) imaging. Methods:[18F]FPTP2 was prepared by substituting tosyl of precursor with 18F, purified and confirmed by HPLC. [18F] FPTP2 (37 MBq/15 kg) was injected into Chinese mini-swines intravenously by a venous catheter. The cardiac PET scans were performed at 2, 10, 20, 30, 40, 50 and 60 min after injection. Results:The total radio-synthesis time was 70 min, radiochemical yield was 25±7.2% without correction. The radiochemical purities (RCP) were >98% after purification. In PET imaging study, the heart uptake and target-to-nontarget uptake ratios increased with time. The heart/liver and heart/lung ratios were 0.65±0.10 and 3.47±0.29 at 2 min post injection, 0.92±0.13 and 9.28±0.77 at 60 min post injection respectively. Conclusion:Although the higher uptake of [18F]FPTP2 were shown in myocardium, the heart/liver ratio still need to be improved in future study.
    • 吴兴业; 王崇磊
    • 摘要: 以叔丁基肼水溶液、糠氯酸为原料,在甲苯做溶剂、冰乙酸做催化剂条件下经成腙、闭环、脱溶,然后在水相结晶制得高含量2-叔丁基-4,5-二氯-3(2H)-哒嗪酮(以下简称哒嗪酮);哒嗪酮再与对叔丁基苄硫醇在甲醇做溶剂的条件下经缩合、脱甲醇、水相结晶制得高含量哒螨灵原药.反应具有操作稳定、收率高的优点,缩合反应在低温下进行,有利于提高产品质量及收率;哒螨灵在一定浓度的稀碱水溶液中结晶,其含量可达到96%以上.该方法具有产品质量高、成本低的优点,适合工业化生产.
    • 郑玉国; 徐开宇; 孙长梅; 曾凡信; 周青; 周莉; 郭晴晴
    • 摘要: Bichromen-2-one 1 ,3 ,4-oxadiazol-pyridazinone in yield of 68.6%was synthesized by the reaction of 3-(5-mercapto-1,3,4-oxadiazol -2-yl) -2H-chromen-2-one with 2-benzyl-4,5-dichloropyridazin -3(2H)-one using K2 CO3 as the catalyst in DMF at 125°Cfor 6 h.The structure was characterized by 1 H NMR, IR and elemental analysis.%以DMF为溶剂,碳酸钾为催化剂,2-(2H-苯并吡喃-2-酮-3基)-5-巯基-1,3,4-噁二唑与4,5-二氯-2-苄基-哒嗪-3-酮于125°C反应6 h,合成了4-{2-[(2H-苯并吡喃)-2-酮]-1,3,4-噁二唑-5-硫醚}-2-苄基-5-{2-[(2H-苯并吡喃)-2-酮]-1,3,4-噁二唑-5-硫醚}哒嗪-3(2H)-酮化合物,收率68.6%,其结构经1H NMR、 IR以及元素分析确证。
    • 彭程; 牟甜甜; 赵祚全; 马云川; 张现忠
    • 摘要: 设计并合成了一种18F标记哒嗪酮类似物:2-特丁基-4-氯-5-(2-氟[18F]乙氧基)-2H-3-哒嗪酮(18F-FP2),通过生物分布实验评价了其用于心肌灌注显像的可行性.18F-FP2的总制备时间为70~90 min,校正后的放化产率为53.0%士5.2%,放化纯度>98%;18F-FP2为脂溶性化合物,在水溶液中可稳定放置3h以上.生物分布实验结果显示,18F-FP2在肝、肺中初期摄取高,注射后2 min分别为(14.53土2.36)%ID/g和(33.69土10.79)%ID/g,但清除很快,注射后15 min,其肝、肺的清除率已分别达57.7%和86.2%.18F-FP2的心肌摄取较低,最高摄取值为(4.09土0.53)%ID/g(注射后2 min).这可能因标记侧链上未带苯环造成的,说明哒嗪酮侧链的芳环结构对心肌的摄取与滞留有较大影响.%A fluorine-18 labeled pyridazinone derivative: 2-tert-butyl-4-chloro-5-(2-[18F]flu-roethoxy)-2H-pyridazin-3-one (18F-FP2) was designed and prepared as a potential myocar-dial perfusion imaging agent. The total radio-synthesis time was 70-90 min, typical decay-corrected radiochemical yield was 53. 0%±5. 2%, and the radiochemical purities were > 98% after purification. It is a lipophilic compound, and stable in water for 3 h. The results of biodistribution studies in mice showed that 18F-FP2 had high liver and lung uptake at initial post-injection time, the uptake was (14. 53±2. 36)%ID/g and (33. 69±10. 79)%ID/g at 2 min post-injection, respectively. Radioactivity was washed out very fast from liver and lung, the rate of clearance was 57. 7% and 86. 2% at 15 min post-injection, respectively. However the heart uptake of 18F-FP2 was very low, the highest heart uptake was(4. 09± 0. 53)%ID/g at 2 min post-injection. This may due to the removing of phenyl group in the labeling sidechain of pyridazinone, indicating that the aromatic ring has strong influence on the heart uptake and retention.
    • 李建辉; 卫世乾
    • 摘要: 对不同结构6-芳基哒嗪酮的合成方法及其生物活性进行了分类综述,并对发展趋势和应用前景进行了展望.
    • 李洪森; 赵琳静; 汤佳蓉; 成嫕喆; 陈婕; 郑志怡; 孙海琳
    • 摘要: 以4,5-二氯-3(2H)-哒嗪酮和2-溴-1-苯乙酮或2-溴-1-苯-1-丁酮反应合成了中间体4,5-二氯-2-(2-苯基-2-氧代-乙基))-3(2H)哒嗪酮,再与吗啉和哌啶反应合成了标题化合物.所有化学物的结构通过1 HNMR、IR和元素分析确证.初步生物活性测定表明,部分化合物在200mg·L-1对东方粘虫有一定的生物活性.%The mediate 4,5-dichloro-(2-phenyle-2-oxo-ethyl)-3(2H)pyridazinone was synthsized from 4,5-dichloro-3(2H)-pyridazinone with 2-bromo-1-phenylethanone or 2-bromo-1-phenylebutanone, followed by substitued reaction with morpholine and pi-peridine to give the target compounds. All the compounds were confirmed by HNMR, IR and elemental analysis. The preliminary bioassy tests showed that some of the compounds exhibited activity against Oriental armyworm at 200mg · L-1.
    • 熊壮; 李海畅; 梁娜; 尹娟; 卢平; 薛伟
    • 摘要: 设计合成了10个新型的含三元杂环席夫碱类衍生物,所有化合物结构通过1HNMR,13C NMR,IR和元素分析确证,生物活性初步研究结果表明,在50 mg/L浓度下,目标化合物对小麦赤霉菌(G.zeae)、苹果腐烂病菌(C.mandshurica)和辣椒枯萎病菌(F.oxysporum)具有一定的抑制活性.%Ten novel three-ring heterocyclic Schiff-base derivatives were designed and synthesized. Their structures of all these compounds were confirmed by 'H NMR, 13C NMR, IR spectra and elemental analysis. The preliminary result of bioassay showed that the title compounds exhibited some degree of antifungal activities on G. zeae, C. mandshurica and F. oxysporum under 50 mg/L concentration.
    • 郑玉国; 魏学; 郭晴晴; 卢平; 王贞超; 薛伟
    • 摘要: 设计合成了9种未见文献报道的双三唑席夫碱哒嗪酮化合物.用1H NMR、13C NMR、IR及元素分析表征结构.生物活性初步结果表明,在500 mg/L浓度下部分化合物对黄瓜花叶病毒(CMV)、小麦赤霉病菌(G.zeae)、辣椒枯萎病菌(F.oxysporum)和苹果腐烂病菌(C.mandshurica)有一定抑制作用.%Nine novel pyridazinone derivatives containing 1,2,4-triazolo and Schiff base were synthesized. Their structures were characterized by !H NMR, 13C NMR, IR and elemental analyses. The preliminary bioassay showed that, under 500 mg/L concentrations, some of them exhibited certain anti-cucumber mosaic virus (CMV) , G. Zeae, F. Oxysporum and C. Mandshurica activities and fungicidal activities.
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