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《Journal of heterocyclic chemistry》2018,55(7):1574-1578
A series of 1‐azaaurone derivatives were designed and synthesized from 3,5‐dimethoxyaniline and 2‐chloroacetonitrile. Their structures were characterized by melting point, 1H NMR, IR, and elemental analysis, as well as 13C NMR. The target compounds were evaluated for antitumor activities against human hepatocellular liver carcinoma cell line (HepG‐2) and human cervix carcinoma cell line (Hela) using methyl thiazolyl tetrazolium method. The results revealed that several 1‐azaaurones exhibited strong proliferation inhibition efficacy against HepG‐2 and Hela with an IC50 range of 5.6–8.8 μg/mL without damaging normal cell. 相似文献
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Synthesis and Biological Activities of Novel 6‐Alkylamino‐11,12‐dihydro‐11‐arylbenzo[c]phenanthridine Derivatives 下载免费PDF全文
Min Zhang Li Liu Huifeng Xiao Ting Zhao Liuqing Yang Xiaohua Xu 《Journal of heterocyclic chemistry》2016,53(1):234-240
A series of novel benzo[c]phenanthridine derivatives 2a , 2b , 2c , 2d , 2e , 2f , 2g , 2h , 2i , 2j , 2k , 2l , 2m and 3a , 3b , 3c , 3d , 3e , 3f bearing an alkylamino side chain at their 6‐position were synthesized. All of the target compounds were confirmed by 1H NMR, 13C NMR, and HRMS, and some of them were also characterized by IR and 19F NMR. The preliminary bioassays showed that the target compounds displayed fungicidal activities; for example, compound 2l showed 60.0% and 70.0% inhibitive activity against Alternaria solani and Cercospora arachidicola at 50 mg/L, respectively, and some compounds also displayed plant growth‐regulating activities. 相似文献
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Yongqiang Li Ziwen Wang Pengxiang Zhang Yuxiu Liu Lixia Xiong Qingmin Wang 《Journal of heterocyclic chemistry》2014,51(5):1410-1414
To investigate the alkyl analog of insecticide chlorfenapyr, two series of 2‐alkyl‐4‐bromo‐5‐(trifluoromethyl)pyrrole‐3‐carbonitriles were synthesized with a cycloaddition as the key step. The target products were characterized by 1H‐NMR spectroscopy, elemental analysis, or HRMS. The insecticidal, herbicidal, and antifungal activities of the target compounds were evaluated and found that these compounds did not show much insecticidal activity, but compounds 4 , 10 , and 11 had very good fungicidal activities against Alternaria solani and Fusarium oxysporum. Moreover, compound 4 had an outstanding inhibition effect against pigweed. 相似文献
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Akira Hasegawa Yuichi Hioki Etzuko Yamamoto Makoto Kiso Ichiro Azuma 《Journal of carbohydrate chemistry》2013,32(3):359-369
A variety of N-[2-O-(2-acetamido-6-O-acyl-1-S-acyl-2, 3-dideoxy-1-thio-β3-D-glucocyranose-3-yl)-D-lactoyl]-L-alanyl-D-isoglutamine methyl esters were synthesized. Their immunoadjuvant activities were examined in guinea-pigs. 相似文献
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A series of 6′‐chloro‐1′,1′‐dioxo‐2′H‐spiro[benzo[d][1,3,7]oxadiazocine‐4,3′‐(1,4,2‐benzodithiazine)]‐2,6(1H,5H)‐dione derivatives 2a , 2b and 3a , 3b have been synthesized starting from 3‐aminobenzodithiazines 1a , 1b and isatoic anhydride. Subsequent reactions of 2a with 3‐chlorophenyl isocyanate gave condensation products 4 and 5 . Compound 2a was also converted into 3‐(2‐aminobenzamido)‐6‐chloro‐7‐methyl‐1,1‐dioxo‐1,4,2‐benzodithiazine derivatives 6 , 7 , 8 , 9 , 10 . The mechanisms of the reactions are discussed. 相似文献
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利用活性拼接原理, 将喹喔啉引入到杨梅素结构中, 合成了一系列含喹喔啉基团的杨梅素新型衍生物. 采用浊度法测试了目标化合物的体外抑菌活性, 结果表明, 目标化合物对柑橘溃疡病菌(X. Citri)和水稻白叶枯病菌(X. Oryzae)均表现出较好的抑制活性. 目标化合物对柑橘溃疡病菌的抑制活性(EC50)均优于对照药叶枯唑和噻菌铜(EC50分别为54.85和61.13 μg/mL), 其中化合物4o抑制活性(EC50=11.17 μg/mL)最优; 目标化合物对水稻白叶枯病菌的抑制活性EC50均优于对照药叶枯唑和噻菌铜(EC50分别为148.20和175.47 μg/mL), 其中化合物4f抑制活性(EC50=34.49 μg/mL)最优. 采用半叶枯斑法测试了目标化合物的抗烟草花叶病毒(TMV)活性, 结果表明, 所有目标化合物在浓度为500 mg/L时均有一定的抑制作用. 相似文献
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为了寻找结构新颖,活性较好的抗肿瘤化合物,本文设计并合成了15个未见报道的异吲哚酮衍生物(I1~I5, II1~II5和III1~III5),其结构经1H NMR和HR-MS(ESI)表征。使用四甲基偶氮唑盐(MTT)法,初步的生物活性测试结果表明:部分化合物对人肺癌细胞A549(II4, IC50=15.49μM)、人结肠癌细胞Colo205(II4, IC50=15.54μM)、人胰腺癌细胞PNAC-1(II4, IC50=37.07μM)和人骨髓瘤细胞U266(II5, IC50=75.27μM)表现出明显的抑制作用。
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芳氧乙酸-3,3-二甲基-2-羰基丁酯衍生物的合成与生物活性史延年,李士明,方建新(南开大学元素有机化学研究所,天津,300071)关键词芳氧乙酸酯,合成,生物活性芳氧乙酸及其酯类衍生物具有良好的生物活性.作者曾以苯氧乙酸类化合物为母体,合成了一系列... 相似文献
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Michael J. Geier Eric G. Bowes Graham M. Lee Haoxin Li Taryn O'Neill Andrew Flewelling Christopher M. Vogels Andreas Decken Christopher A. Gray Stephen A. Westcott 《Heteroatom Chemistry》2013,24(2):116-123
A family of arylspiroborate compounds has been prepared from 2,3‐dihydroxynaphthalene and characterized fully using multinuclear NMR spectroscopy and elemental analyses. Single crystal X‐ray diffraction studies were carried out on the tetramethylammonium ( 4 ) and calcium ( 6 ) derivatives. Compound 6 represents the first structurally characterized example of a calcium arylspiroborate salt. All compounds showed modest antifungal and antimycobacterial activities. These results have revealed a new class of compounds that should be further developed to design more potent and selective antitubercular agents. © 2013 Wiley Periodicals, Inc. Heteroatom Chem 24:116–123, 2013; View this article online at wileyonlinelibrary.com . DOI 10.1002/hc.21072 相似文献
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《Journal of heterocyclic chemistry》2017,54(6):3241-3249
New derivatives of 2,5‐dimercapto‐1,3,4‐thiadiazole substituted both at one or two exocyclic sulfur atoms with a series of aroyl or ethoxycarbonyl groups were synthesized in reactions of 2,5‐dimercapto‐1,3,4‐thiadiazole salts with appropriate acid chlorides or ethyl chloroformate in mild conditions. The products were characterized by spectroscopy (1H NMR, 13C NMR, IR, and HRMS). Some from the synthesized compounds were screened in vitro and in vivo for antibacterial and antifungal activities against a panel of reference strains of microorganisms. The study revealed that ethyl S‐(5‐mercapto‐1,3,4‐thiadiazol‐2‐yl) carbonothioate seems to be the most active and versatile compound against Gram‐positive bacteria, Gram‐negative bacteria, and plant pathogenic fungi. 相似文献
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《中国化学》2018,36(7):635-638
A convenient and practicable method for the synthesis of the novel 2‐(trifluoromethyl)‐6‐arylimidazo[2,1‐b][1,3,4]‐thiadiazole (bis‐)Mannich base derivatives containing various substitutedpiperazine motif has been developed based on the fused‐heterocycle intermediate. The new structures were identified through melting points, 1H NMR, 13C NMR, 19F NMR, elemental analysis (or HRMS) and X‐ray single‐crystal diffraction. The pesticidal bioassays showed that some of compounds exhibited good fungicidal activities against Cercospora arachidicola, Physalospora piricola and Rhizoctonia cereali at 50 mg/L; some of them displayed favourable insecticidal activities against oriental armyworm (Mythimna separata Walker) at 200 mg/L, particularly, Vk and Vm with mortality rate of 75% and 80% respectively, could be considered as new insecticidal lead compounds for further structural optimization. 相似文献
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Marina O. Shibinskaya Nina A. Kutuzova Alexandr V. Mazepa Sergey A. Lyakhov Sergey A. Andronati Mykhayl Ju. Zubritsky Valerij F. Galat Janusz Lipkowski Victor Ch. Kravtsov 《Journal of heterocyclic chemistry》2012,49(3):678-682
A series of 6‐(3‐aminopropyl)‐6H‐indolo[2,3‐b]quinoxalines were synthesized with high yields by the reaction of 6‐(3‐chloropropyl)‐6H‐indolo[2,3‐b]quinoxaline and corresponding amines in presence of tetrabutylammonium iodide in boiling toluene or dimethylformamide at room temperature. It was found that boiling of 6‐(3‐chloropropyl)‐6H‐indolo[2,3‐b]quinoxaline in acetone with sodium iodide or in acetic acid lead to intramolecular cyclization product. 相似文献
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Shu‐Jun Chao Xin‐Ping Hui Shuo Li Zao‐Zao Qiu Peng‐Fei Xu Zi‐Yi Zhang Qin Wang Zuo‐Wu Guan 《中国化学会会志》2005,52(3):539-544
Several new 5‐[4′‐(5‐phenyl‐1,3,4‐oxadiazol‐2‐ylsulfanylmethyl)‐biphenyl‐2‐yl]‐tetrazoles derivatives have been synthesized. The structures of these new compounds were confirmed by elementary analyses and spectral data. The antibacterial activities of the compounds were also evaluated. 相似文献
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Synthesis and Antifungal Activities of Some New 5,7‐Disubstituted[1,2,4]Triazolo[1,5‐a]Pyrimidin‐6‐one Derivatives 下载免费PDF全文
Susanta Kumar Borthakur Sukanya Borthakur Debarshi Goswami Paran Boruah Pabitra Kumar Kalita 《Journal of heterocyclic chemistry》2016,53(6):2079-2083
Synthesis of a new series of [1,2,4]triazolo[1,5‐a]pyrimidin‐6‐one by [4 + 2]cycloaddition reaction of 3‐benzylidineamino[1,2,4]triazole with monophenyl ketene and diphenyl ketene generated in situ from phenylacetyl chloride and diphenylacetyl chloride in the presence of triethylamine is described. The newly synthesized compounds were also tested for antifungal activities against Rhizoctonia solani and Trichoderma sp. 相似文献
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Synthesis and Herbicidal Evaluation of 3‐N‐Substituted Amino‐6‐benzyloxypyridazine Derivatives 下载免费PDF全文
Min Zhang Fang‐Zhong Hu Ting Zhao Liu‐Qing Yang Hua‐Zheng Yang 《Journal of heterocyclic chemistry》2014,51(5):1404-1409
A variety of 3‐N‐substituted amino‐6‐benzyloxypyridazine derivatives were designed and synthesized in satisfactory yields. Their structures were confirmed by IR, 1H‐NMR, and elemental analysis; compound 5j was further determined by X‐ray diffraction crystallography. Their herbicidal activities were evaluated through barnyard grass and rape cup tests in laboratory bioassays. Most of the title compounds 5 displayed moderate herbicidal activities against the dicotyledonous plant Brassica campestris L. The most active compounds in the laboratory were also evaluated in the greenhouse. 相似文献
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