共查询到19条相似文献,搜索用时 78 毫秒
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3-乙酰基-2-芳基-5-(6-吲哚基)-1,3,4-噁二唑啉化合物的微波合成及表征 总被引:1,自引:0,他引:1
噁二唑啉化合物由于具有杀虫[1],杀菌[2],抗艾滋病毒[3]等生物活性受到药物化学家的广泛关注.而吲哚因独特的化学结构使其衍生出的化合物显示出重要的生物活性,如抗疟疾[4]、抗肿瘤[5]、抗糖尿病[6]等,可以用作HT受体抑制剂[7]、环氧酶抑制剂[8]等.鉴于不同活性的基团在同一分子中聚集能明显改善化合物的生物活性这一特性,本文将吲哚引入到噁二唑啉化合物中,以期实现活性的叠加,从而发现新的生物活性更好的化合物. 相似文献
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微波辐射下,以芳香醛和芳香酮为起始原料合成2,4,6-三芳基吡喃盐,在NaOH水溶液中与盐酸羟胺发生开环、缩环和脱苯甲酰基反应,一步生成3,5-二芳基异噁唑衍生物。考察了微波辐射功率和辐射时间对目标产物收率的影响,2,4,6-三芳基吡喃盐与盐酸羟胺反应生成3,5-二芳基异噁唑衍生物的最佳微波辐射功率为600W,辐射时间为8min,最大收率为83%。该法不仅避免了使用高氯酸造成的环境污染,而且以水作为反应介质,使后处理简便。该工艺具有操作安全、反应条件温和和产率高等优点,是一种环境友好的合成工艺。产物经元素分析、1HNMR和MS测试技术表征了其结构。 相似文献
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以N-羟基-4-甲氧基苯甲醛肟氯化物为原料,经两步反应制得3-对甲氧基苯基-5-甲基-异噁唑-4-甲酰肼(3);3依次经缩合和环合反应合成了一系列新型的2-芳基3-乙酰基-5-(3-对甲氧基苯基-5-甲基-异噁唑-4-基)-Δ4-1,3,4-噁二唑啉衍生物,其结构经~1H NMR,13C NMR,IR,MS(EI)和元素分析表征。 相似文献
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含氟1,3,4-噁唑啉和1,3,4-噁二唑类化合物的合成及其抗癌活性 总被引:1,自引:0,他引:1
对氟苯甲酰腙与乙酸酐或丙酸酐反应后再脱水环化制得2-苯基-3-乙酰基-5-对氟苯基-1,3,4-噁唑啉(3)或2-苯基-3-丙酰基-5-对氟苯基-1,3,4-噁唑啉(4).N-对氟苯甲酰基-N′-苯甲酰肼在POCl3存在下脱水环化制得2-苯基-5-对氟苯基-1,3,4-噁二唑(6).新化合物3,4和6的结构经1H NMR,IR,MS和元素分析表征.用MTT方法评价了其对HepG-2,A549-1和231-2癌细胞株的体外生长抑制活性.结果表明,3,4和6均具有潜在的体外抑制癌细胞生长活性,其中3的活性最强. 相似文献
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Synthesis and Their Endothelium Vascular Relaxation of Arecoline Derivatives Containing Oxadiazoline
Ten novel 1,1-dimethyl-3-(2-or 5-aryl-4-acetyl-2,3-dihydro-1,3,4-oxadiazoline-5-or-2-yl)-1,2,5,6-tetrahydropyridinium iodides were synthesized from starting materials nicotinalde-hyde or nicotinic acid by two different synthetic methods respectively. The preliminary bioactive tests indicate som compounds exhibit potent relaxing effect on endothelial cells, comparable to Ach or arecoline. 相似文献
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Synthesis and Biological Activities of Some New Annulated Pyrazolopyranopyrimidines and Their Derivatives Containing Indole Nucleus 下载免费PDF全文
Anand R. Saundane Prabhaker Walmik Manjunatha Yarlakatti Vijaykumar Katkar Vaijinath A. Verma 《Journal of heterocyclic chemistry》2014,51(2):303-314
The key intermediate 6‐amino‐3‐methyl‐4‐aryl‐1‐(5′‐substituted‐3′‐phenyl‐1H‐indol‐2′‐carbonyl)‐1,4‐dihydropyrano[2,3‐c]pyrazol‐5‐carbonitriles 3a , 3b , 3c , 3d , 3e , 3f , 3g , 3h , 3i , 3j , 3k , 3l , 3m , 3n , 3o were prepared by cyclocondensation of 3‐methyl‐1‐(5′‐substituted‐3′‐phenyl‐1H‐indol‐2′‐carbonyl)‐5‐(4H)‐pyrazolones 1a , 1b , 1c with arylidine derivatives of malononitrile 2a , 2b , 2c , 2d , 2e . The compounds 3a , 3b , 3c , 3d , 3e , 3f , 3g , 3h , 3i , 3j , 3k , 3l , 3m , 3n , 3o were subjected to cyclocondensation reaction with formamide, formic acid, and carbon disulfide to afford the title compounds 4a , 4b , 4c , 4d , 4e , 4f , 4g , 4h , 4i , 4j , 4k , 4l , 4m , 4n , 4o , 5a , 5b , 5c , 5d , 5e , 5f , 5g , 5h , 5i , 5j , 5k , 5l , 5m , 5n , 5o , and 6a , 6b , 6c , 6d , 6e , 6f , 6g , 6h , 6i , 6j , 6k , 6l , 6m , 6n , 6o , respectively. The structures of all these previously unknown compounds were confirmed by their spectral studies and elemental analysis. These compounds were screened for their antimicrobial and antioxidant activities. 相似文献
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《Journal of heterocyclic chemistry》2018,55(6):1382-1390
A series of novel quinazolinone acylhydrazone derivatives containing the indole moiety were designed, synthesized, and evaluated for their inhibition activities against some important phytopathogens in vitro. Antibacterial experiments indicated that some compounds exhibited remarkable inhibition activities against tested bacteria. Especially, the EC50 values of 7a (EC50 = 55.13 μg/mL against Xoo, EC50 = 56.92 μg/mL against Rs) demonstrated the best antibacterial activities against Xoo and Rs than the other compounds, and the control agents Bismerthiazol (EC50 = 89.80 μg/mL against Xoo) and Thiodiazole copper (EC50 = 189.52 μg/mL against Rs), moreover, compound 7o (EC50 = 50.80 μg/mL) displayed the excellent activity against Xac than the control Bismerthiazol (EC50 = 56.92 μg/mL). 相似文献
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从苔藓虫Zoobotryon pellucidum中提取的2,5,6-三溴-1-甲基芦竹碱(TBG)能较好地抑制海洋生物藤壶的附着. 为提高该类化合物在防污涂料中的复配性能, 合成了4个新型的不同卤素取代和N-取代且具有较好亲脂性能的TBG类似物. 通过1H NMR, 13C NMR, IR和元素分析对目标化合物6a~6d进行了结构表征. 生物实验结果表明, 化合物5~6对海藻Nitzschia closterium均具有较好的生长抑制活性, 其中以亲脂性较强的6b和6d抑制作用最为显著, LC50分别可达1.33 µg/mL和1.06 µg/mL. 对化合物的定量构效关系进行了初步探讨. 相似文献
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为了发现高活性的抗病毒化合物,以蓝刺头碱为先导,运用骨架跃迁策略,设计合成了15个含有酰腙吲哚片段的蓝刺头碱衍生物,并通过1H NMR、13C NMR和HRMS确证了其结构,研究了其对烟草花叶病毒(TMV)的钝化、治疗和保护活性。研究结果表明,部分化合物具有较高的抗TMV活性。其中,化合物4n(43.5%,40.1%,38.7%)抗TMV的钝化、治疗和保护活性高于病毒唑(38.6%,36.5%,37.2%)和先导化合物L2(40.5%,34.7%,38.3%)。化合物4d(40.8%)、4f(42.0%)对TMV的钝化活性优于病毒唑(38.6%)和先导化合物L2(40.5%)。化合物4I(38.4%)对TMV的钝化活性与病毒唑(38.6%)相当。化合物4f(36.4%)对TMV的保护活性与病毒唑(37.2%)相当。化合物4n有望成为一种潜在的抗病毒农药。 相似文献
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Microwave-Assisted Solid-Phase Synthesis of Cephalosporin Derivatives with Antibacterial Activity 总被引:1,自引:0,他引:1
Mazaahir Kidwai Preeti Misra Kumar R. Bhushan Rajendra K. Saxena Meena Singh 《Monatshefte für Chemie / Chemical Monthly》2000,131(9):937-943
Summary. The reaction of heterocyclic acids with 7-amino-cephalosporanic acid adsorbed on basic alumina under microwave irradiation
afforded the N-acylated cephalosporin analogues in satisfactory yield. All compounds were tested for their antibacterial activity;
some of them showed significant antibacterial properties. Cefotaxime and cephalothin were used as reference drugs.
Received February 23, 2000. Accepted March 28, 2000 相似文献
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Mazaahir Kidwai Preeti Misra Kumar R. Bhushan Rajendra K. Saxena Meena Singh 《Monatshefte für Chemie / Chemical Monthly》2000,12(1):937-943
The reaction of heterocyclic acids with 7-amino-cephalosporanic acid adsorbed on basic alumina under microwave irradiation afforded the N-acylated cephalosporin analogues in satisfactory yield. All compounds were tested for their antibacterial activity; some of them showed significant antibacterial properties. Cefotaxime and cephalothin were used as reference drugs. 相似文献