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《化学研究》2015,(4)
苯胺或取代苯胺、二硫化碳与水合肼在氢氧化钾催化下经加成与取代反应合成了10种N(4)-取代氨基硫脲,随后在浓盐酸催化下分别与2-羟基-1-萘甲醛加成合成了10种未见报道的2-羟基-1-萘甲醛缩-N(4)-取代氨基硫脲.通过IR、1 H NMR与13 C NMR对标题化合物进行了结构表征;采用离体法初步测试了标题化合物对6种常见农作物真菌病源菌的抑菌活性,并推测其可能的构效关系.结果表明,标题化合物对水稻纹枯病菌、小麦赤霉病菌、番茄早疫病菌、黄瓜枯萎病菌、马铃薯晚疫病菌及辣椒疫霉病菌均表现出一定的抑菌活性,其抑菌活性大小与标题化合物N(4)-取代基中苯环所连取代基的类型与位置有关. 相似文献
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为了寻找生物活性良好的噻唑基丙烯腈类化合物, 利用2-[4-(2,6-二氟苯基)噻唑-2-基]乙腈(3)分别与取代氯甲酸酯4和取代苯基异氰酸酯6在碱存在下反应, 合成了8个2-[4-(2,6-二氟苯基)噻唑-2-基]-3-羟基-3-烃氧基丙烯腈化合物5和7个2-[4-(2,6-二氟苯基)噻唑-2-基]-3-羟基-3-取代苯胺基丙烯腈化合物7, 均为首次报道的丙烯腈类化合物. 化合物结构经1H NMR, IR, MS和元素分析表征. 初步生物活性测定结果表明, 在试验浓度下, 目标化合物均具有一定的杀虫和抑菌活性, 其中化合物5f和5h在100 mg/L浓度下对炭疽病菌的抑制率达95%; 化合物5g和7d在250 mg/L浓度下对棉红蜘蛛的致死率达85%. 相似文献
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利用Hantzsch反应合成了13个N-芳基-4-(吡啶-2-基)-5-(1H-1,2,4-三唑-1-基)噻唑-2-胺衍生物,所有化合物的结构均经1H NMR,MS及元素分析确证.研究发现,溶剂对不同取代基的目标化合物的合成影响很大.生物活性测试结果表明,化合物均具有一定的杀菌活性.其中,化合物6c对番茄早疫和苹果轮纹、化合物6g对番茄早疫、化合物6h对黄瓜黑腥及化合物6i对苹果轮纹均显示80%以上的杀菌活性. 相似文献
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设计合成了系列光系统II (PS-II)电子传递抑制剂2-氰基-3-(2-氟吡啶-5-基)甲氨基-3-甲硫基氰基丙烯酸酯类化合物. 其结构经1H NMR、元素分析确证. 生物活性测定表明: 部分化合物显示出很好的除草活性. 其中活性最好的化合物在150 g/ha, 对阔叶杂草的防效在90%以上. 构效关系研究表明: 氰基丙烯酸酯的3位取代基对它们的活性影响较大. 3位由(2-氟吡啶-5-基)甲氨基取代的氰基丙烯酸酯和相应的氯取代的氰基丙烯酸酯的除草活性相当或稍高. 相似文献
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The title compound N 1-(1,3,4-thiadiazole-2-yl)-N 3-m-chlorobenzoyl-urea (C 9 H 7 N 4 OSCl,M r=254.70) was prepared by the reaction of m-chlorophenyl isocyanate with 2-amino-1,3,4-thiadiazole in dry acetonitrile.The effect of the title compound on tumor metastasis was analyzed by Lewis-lung-carcinoma model.The bioassay showed that the title compound significantly reduced the number of lung metastasis.The crystal structure has been determined by X-ray diffraction.The crystal belongs to the monoclinic system,space group P2 1 /c with a=11.565(2),b=9.5616(19),c=10.221(2),β=111.75(3)°,Z=4,V=1049.8(4)3,D c=1.612 Mg/m 3,F(000)=520,μ(MoKa)=0.544 mm-1,R=0.0468 and wR=0.0922 for 1236 observed reflections (I > 2σ(I)). 相似文献
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Purification of the cytotoxic fractions of the methanol extracts of Kalanchoe hybrida leads to three new compounds with the basic skeleton of α-pyrone ring-opening products of bufadienolides, namely, kalanhybrin A-C (1-3). Moreover, four bufadienolides (4-7) and eight other compounds were also characterized from the title plant. The isolated compounds (1-7) were evaluated for their cytotoxicity toward MCF-7, NCI-H460, and SF-268 tumor cell lines. Among them, compounds 4 and 6 displayed significant cytotoxicity toward MCF-7 and NCI-H460 tumor cell lines at the tested concentration. In addition, the biosynthetic pathway of these α-pyrone ring-opening derivatives was also proposed. 相似文献
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IntroductionTrinitrobenzenes(TNBs)havebeenthefocusofanumberofinvestigationsforalongtime.Manyoftheirderivatives,forexamplemeth... 相似文献
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he molecular geometries, heats of formation, electronic structures of three trinitrobenzenes(1,2,3-TNB, 1,2,4-TNB, 1,3,5-TNB), their chloro derivatives were studied by using the quantum chemical MO AM1 method at the RHF level, ab initio method at the HF/3-21G level. The decompositions of the title compounds were investigated by using the AM1 method at the UHF level. The decomposition activation energies were obtained, the order of the relative stabilities of the title compounds is found. The substituent effects on the structures, properties, on the decompositions of the title compounds are discussed in the present paper. 相似文献
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α-芳甲酰基烯酮二硫缩醛的新合成方法 总被引:1,自引:0,他引:1
以碳酸钾为碱,芳甲酰丙酮(1)与二硫化碳、卤代烃反应得到2-乙酰基-2-芳甲酰基烯酮硫代缩醛(2),2在乙硫醇钾作用下脱乙酰基生成标题化合物(3)。1→3的转化具有反应条件温和、产物产率高及对3中各种缩醛基均可通用等特点。 相似文献
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2',3'-O-异亚丙基-5'-O-[N,N-二(2-氯乙基)磷酰胺基]核苷的合成陈茹玉,迟国臣,陈小茹(南开大学元素有机化学研究所,天津,300071)关键词核苷,亚磷酰化,抗肿瘤活性很多核苷类化合物具有很好的抗肿瘤、抗病毒等生物活性,某些化合物已... 相似文献
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Abdel-Rahman Farghaly Hussein El-Kashef 《Monatshefte für Chemie / Chemical Monthly》2006,137(9):1195-1202
Summary. The syntheses of the title heterocycles were achieved using 5-amino-1-(1-benzyl-1H-indol-3-ylcarbonyl)-1H-pyrazole-4-carbonitrile as starting material. These compounds were converted into the 4-imidazolinyl derivatives which were
subjected to cyclization reactions to afford the title compounds. 相似文献
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Abdel-Rahman Farghaly Hussein El-Kashef 《Monatshefte für Chemie / Chemical Monthly》2006,44(6):1195-1202
The syntheses of the title heterocycles were achieved using 5-amino-1-(1-benzyl-1H-indol-3-ylcarbonyl)-1H-pyrazole-4-carbonitrile as starting material. These compounds were converted into the 4-imidazolinyl derivatives which were
subjected to cyclization reactions to afford the title compounds. 相似文献