共查询到20条相似文献,搜索用时 15 毫秒
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以3,4,5-三甲氧基苯甲酸为原料,经过Claisen缩合等反应设计合成一系列新的噻唑并[3,2-b][1,2,4]三唑-6-酮稠杂环衍生物并测定其体外抗肿瘤活性。目标化合物经~1HNMR、~(13)CNMR和高分辨质谱等表征后,在He La、HCT116、BEL-7402及L-02细胞中用MTT法测定其抑制细胞增殖的程度,并初步判断化合物的体外抗癌活性。结果表明,与临床常用药顺铂(DDP)相比,多数化合物具有抑制肿瘤细胞增殖活性。其中,5-(4-苄氧基苯亚甲基)-2-(3,4,5-三甲氧基苯基)噻唑并[3,2-b][1,2,4]三唑-6(5H)-酮、5-(4-乙酰氧基苯亚甲基)-2-(3,4,5-三甲氧基苯基)噻唑并[3,2-b][1,2,4]三唑-6(5H)-酮、5-(α-呋喃亚甲基)-2-(3,4,5-三甲氧基苯基)噻唑并[3,2-b][1,2,4]三唑-6(5H)-酮和5-(α-噻吩亚甲基)-2-(3,4,5-三甲氧基苯基)噻唑并[3,2-b][1,2,4]三唑-6(5H)-酮对HCT116等3种癌细胞的抑制率高于正常细胞L-02,且对癌细胞有选择性抑制作用,而对正常细胞无毒性,具有良好的后续研究价值。5-(4-氟苯亚甲基)-2-(3,4,5-三羟苯基)噻唑并[3,2-b][1,2,4]三唑-6(5H)-酮对BEL-7402等细胞的抑制率有大幅度提高,但对L-02正常细胞的毒性更大。 相似文献
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为寻找高活性的乙酰胆碱酯酶(AChE)抑制剂,以取代的苯甲醛和N-乙酰甘氨酸为原料经过五步反应合成了13个2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮类化合物,目标化合物结构经1H NMR,13C NMR和HRMS确认。采用Ellman法测试了化合物在10 μmol/L浓度下对AChE的抑制活性,结果显示所有目标化合物均具有抑制活性,其中化合物6-(4-甲氧基苄基)-2-(4-甲氧基苯亚甲基)-2H-噻唑并[3,2-b]-1,2,4-三嗪-3,7-二酮(Ⅴk)活性最好,抑制率达到80.1%。通过分子对接研究了化合物Ⅴk和AChE的结合模式,Ⅴk可以跟AChE的多个催化位点结合。2H-噻唑[3,2-b][1,2,4]三嗪-3,7-二酮类化合物可以为开发具有自主知识产权的新型AChE抑制剂提供参考。 相似文献
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Tarik E. Ali Mohamed A. Assiri Somaia M. Abdel-Kariem Ibrahim S. Yahia 《Journal of Sulfur Chemistry》2018,39(5):472-482
A number of 6-methyl-5-phenyl-2-sulfido-1,2,3,5-tetrahydro-4H[1,2]oxazolo[4′,5′: 5,6]pyrano[2,3-d][1,3,2]diazaphosphinines 4–11 were synthesized via an interaction of tetraphosphorus decasulfide and Lawesson’s reagent under different conditions with 6-amino-3-methyl-4-phenyl-4H-pyrano[3,2-d][1,2]oxazole-5-carbonitrile (3). The reaction mechanisms for these products were discussed. Structures of the newly synthesized products were established on the basis of elemental analysis and spectral data. 相似文献
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Farag M. A. Altalbawy 《International journal of molecular sciences》2013,14(2):2967-2979
The title compounds were prepared by reaction of 1,1′-(5-methyl-1-phenyl-1H-pyrazole-3,4-diyl)diethanone (1) with different aromatic aldehydes 2a–c, namely Furfural (2a), 4-chlorobenzaldehyde (2b) and 4-methoxybenzaldhyde (2c) to yield the corresponding α,β-unsaturated ketones 3a–c. Compound 3 was reacted with malononitrile, 2-cyanoacetamide or 2-cyanothioacetamide yielded the corresponding bis[2-amino-6-(aryl)nicotinonitrile] 4a–c, bis[6-(2-aryl)-2-oxo-1,2-dihydropyridine-3-carbonitrile] 5a–c or bis[6-(2-aryl)-2-thioxo-1,2-dihydropyridine-3-carbonitrile] 6a,b, respectively. The reaction of compound 6a with each of 2-chloro-N-(4-bromophenyl) acetamide (7a), chloroacetamide (7b) in ethanolic sodium ethoxide solution at room temperature to give the corresponding 4,4′-(5-methyl-1-phenyl-1H-pyrazole-3,4-diyl)bis-6-(2-furyl)thieno[2,3-b]pyridine-2-carboxamide] derivatives 9a,b. While compound 6a reacted with hydrazine hydrate yielded the 4,4′-(5-methyl-1-phenyl-1H-pyrazole-3,4-diyl)bis[6-(2-furyl)-1H-pyrazolo[3,4-b]pyridin-3-amine] 11. The structures of the products were elucidated based on their spectral properties, elemental analyses and, wherever possible, by alternate synthesis. Antimicrobial evaluation of the products was carried out. 相似文献
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介绍了在碱催化条件下以对硝基苯甲腈为起始原料,醇解生成对硝基苯甲亚胺酸甲酯,继而氨化、肟化一锅反应,并采用氢化还原的方法最终合成2-(4-氨基苯基)-6-叔丁基-1H-吡唑[1,5-b][1,2,4]三唑,总收率达68.6%。 相似文献
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Toktam Afrough Hossein Eshghi Javad Tajabadi Joel Mague 《Journal of Sulfur Chemistry》2019,40(3):265-276
Several derivatives of the novel tricyclic system ‘dipyrimido[2,1-b:4′,5′-d][1,3]thiazine’ were synthesized via inter- and intramolecular heterocyclization of 2,4-dichloro-5-(chloromethyl)-6-methylpyrimidine and 6-amino-4-aryl-2-thioxo-1,2,3,4-tetrahydropyrimidine-5-carbonitrile in short reaction times under mild conditions. An x-ray analysis together with computational calculations was performed to gain an in-depth understanding of regioselectivity of the reaction. 相似文献
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基于3,6,7-三硝胺[1,2,4]三唑[4,3-b][1,2,4]三唑高能分子与3,4,5-三氨基-1,2,4-三唑,制备了双3,4,5-三氨基-1,2,4-三唑含能离子盐,收率76%。采用红外、质谱、核磁、元素分析等表征了产物结构,检测并计算了该含能盐的物化性能,其分解温度171℃,密度1.77 g/cm3,撞击感度6 J,摩擦感度120 N,计算爆速与爆压分别为8785 m/s和31.5 Gpa。 相似文献
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以6,7-二溴-2,3-二氢苯并[b][1,4]二噁烯为原料,在正丁基锂(n-BuLi)作用下,得到苯炔中间体,再与呋喃发生Diels-Alder反应,得到目标化合物2,3,6,9-四氢-6,9-环氧萘[2,3-b][1,4]二噁烯,通过~1HNMR和ESI-MS对其结构进行确证,并对反应条件进行研究。确定最佳反应条件为:n(6,7-二溴-2,3-二氢苯并[b][1,4]二噁烯)∶n(呋喃)=1∶4、正丁基锂用量为n(n-BuLi)∶n(6,7-二溴-2,3-二氢苯并[b][1,4]二噁烯)=1.2∶1、反应溶剂为甲苯、室温反应20 min,在此条件下,产物收率为76.5%。 相似文献
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咪唑并[1,2-b]哒嗪 总被引:2,自引:0,他引:2
付春 《精细与专用化学品》2005,13(5):14-15
介绍了咪唑并[1,2-b]哒嗪的合成方法、用途、生产及需求.以3,6-二录哒嗪为原料,经氨化、环合、脱氯得咪唑并[1,2-b]哒嗪。咪唑并[1,2-b]哒嗪是合成头孢类抗生素的侧链中间体,因合成难度较大,成为国内开发头孢唑兰的瓶颈. 相似文献
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以三乙胺为催化剂,1-亚硝基-2-萘酚和1,3,3,-三甲基-2-亚甲基吲哚啉为原料合成了N-甲基-3,3-二甲基螺[2H-吲哚-2,3,-[3H]萘并[2,1-b][1,4]噁嗪]。本反应在无溶剂下的微波反应,相比传统有机反应大大缩短了反应时间。并且探讨了反应温度、反应时间、催化剂用量对反应的影响。对产物进行了IR、~1HNMR、~(13)CNMR等表征,结果表明:反应温度150℃,反应10 min,可以获得较高产率的纯产物。 相似文献
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《Journal of Sulfur Chemistry》2013,34(3):363-372
An efficient synthesis of novel spiro(imidazo[4′,5′:4,5′]benzo[1,2-e][1, 4]thiazepine)-9,3′-indolines has been accomplished from 5-amino-2-mercapto benzimidazole, istains and mercapto acetic acid. Compounds 6 were characterized by IR, 1H NMR, 13C NMR and mass spectral data. The title compounds 6a–6e were evaluated for their antimicrobial, anti-inflammatory and antioxidant activity. Compounds 6a–6e exhibited significant antimicrobial activity, and as potent anti-inflammatory and antioxidant activities as that shown by standard drugs. 相似文献
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以1,10-菲咯啉为原料经过三步反应合成得到5,6-二胺-1,10-菲咯啉,常温下5,6-二胺-1,10-菲咯啉与苯偶酰反应生成目标产物2,3-二苯基吡嗪[2,3-f][1,10]菲咯啉,并通过红外、核磁图对其进行了表征。 相似文献
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以C60、邻-硝基苯甲醛和甘氨酸为原料,经过1,3-偶极环加成反应得到2-(2-硝基苯基)吡咯烷[3′,4′∶1,2][60]富勒烯(NPF)。经紫外可见光谱、红外光谱、质谱、核磁共振谱等检测手段鉴定了NPF的结构。通过正交试验研究了反应物物质的量比、温度、时间和溶剂体积等对NPF产率的影响。结果表明,合成NPF的最佳工艺条件为:反应物物质的量比n(C60)∶n(邻-硝基苯甲醛)∶n(甘氨酸)为1∶4∶6,温度为80℃,反应时间为48h,溶剂甲苯体积为70mL,此时产率达81.2%(以消耗的C60计)。 相似文献
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Yangjun Xia Yuanyuan Gao Yong Zhang Junfeng Tong Jianfeng Li Huijuan Li Dejia Chen Duowang Fan 《Polymer》2013,54(2):607-613
An alternating conjugated polymer derived from 4,4,9,9-tetra(4-octyloxyphenyl)indaceno[1,2-b:5,6-b′]dithiophene and thieno[3,2-b]thiophene was synthesized by Stille coupling reaction. The copolymer shows extensive absorption from 360 nm to 590 nm with optical band gap of 2.12 eV. The highest occupied molecular orbit (HOMO) and the lowest unoccupied molecular orbit (LUMO) energy levels of the copolymer, determined by cyclic voltammetry (CV), are about ?5.29 eV and ?3.01 eV, respectively. A field-effect hole mobility of 8.1 × 10?4 cm2/(V s) and an on/off ratio of 2.0 × 103 are obtained in the field-effect transistors based on the copolymer. The Jsc, Voc and FF of the polymer photovoltaic cells (PVCs) based on the copolymer were enhanced simultaneously via the inserting of alcohol soluble conjugated polymer interlayer between active layer and metal cathode, and the maximal power conversion efficiency of 4.19% was achieved in the modified devices under an AM 1.5 simulator (100 mWcm?2). 相似文献