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噁二唑肟醚取代的均三唑水杨醛席夫碱衍生物的合成及抗菌活性 总被引:1,自引:0,他引:1
4-氨基-3-苯基-5-巯基-均.三唑(1)在无水乙酸钠作用下与β-氯苯丙酮(2)缩合得氨基三唑硫基苯丙酮(3).化合物3与盐酸羟胺肟化得羰基肟化物(4),采用氯甲基(噁)二唑(5)对化合物4的肟羟基醚化得均三唑席夫碱(噁)二唑肟醚(6a~6e).肟化物6a~6e与水杨醛缩合得到目标物席夫碱7a~7e.初步的体外抗菌实验表明,席夫碱肟醚类化合物7a~7e的活性明显高于氨基肟醚类化合物6a~6e,且对革兰氏阳性(Sa)的活性高于对革兰氏阴性菌(Ec)的. 相似文献
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2—芳基—5—巯基—1,3,4—三唑衍生物的合成 总被引:1,自引:2,他引:1
报道了7种双(2-芳基-1,3,4-三唑-5-基)二硫化物(2a ̄2g)和5种1-乙基-2-芳基-1,3,4-三唑-5-乙硫醚的合成。化合物结构经元素分析、红外光谱、核磁共振氢谱及质谱确证。生物活性测定结果表明,2b和3b具有较强的抗菌活性。 相似文献
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为发现氟喹诺酮由抗菌活性向抗肿瘤活性转化的结构修饰方法,基于生物电子等排药物设计原理,用唑杂环作为氧氟沙星(1)C-3羧基的等排体、硫醚酮缩氨基硫脲为其功能侧链修饰基,设计合成C-3均三唑硫醚酮缩氨基硫脲目标化合物(6a~6g),其结构经元素分析和光谱数据确证。 体外抗肿瘤活性结果表明,中间体C-3均三唑硫醚酮(5a~5g)和目标化合物(6a~6g)的活性均强于母体氧氟沙星的活性,其中缩氨基硫脲的活性强于相应硫醚酮的活性,尤其是苯环含硝基和氟原子目标化合物的活性与对照药阿霉素的活性相当。 因此,功能缩氨基硫脲链修饰的均三唑作为C-3羧基的等排体有利于提高氟喹诺酮的抗肿瘤活性。 相似文献
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We review our research on the synthesis and study of the physical and biological properties of furyl- and thienylgermatranes and -silatranes.Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 725–732, June, 1992. 相似文献
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David W. Murhammer 《Applied biochemistry and biotechnology》1991,31(3):283-292
The use of the insect cell/baculovirus expression system for producing recombinant proteins of bacterial, plant, insect, and mammalian origin has become widespread. The popularity of this eukaryotic expression system is due to many factors, including (1) potentially high protein expression levels, (2) ease and speed of genetic engineering, (3) ability to accommodate large DNA inserts, (4) protein processing similar to higher eukaryotic cells (e.g., mammalian cells), and (5) ease of insect cell growth (e.g., suspension growth). The following review of the literature discusses two engineering aspects of recombinant protein synthesis by insect cell cultures: bioreactor scale-up and insect cell line selection. Following this review patent abstracts and additional literature pertaining to expression of recombinant proteins in insect cell culture are listed. 相似文献
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Karadakov PB 《The journal of physical chemistry. A》2008,112(31):7303-7309
The aromaticity and antiaromaticity of the ground state (S 0), lowest triplet state (T 1), and first singlet excited state (S 1) of benzene, and the ground states (S 0), lowest triplet states (T 1), and the first and second singlet excited states (S 1 and S 2) of square and rectangular cyclobutadiene are assessed using various magnetic criteria including nucleus-independent chemical shifts (NICS), proton shieldings, and magnetic susceptibilities calculated using complete-active-space self-consistent field (CASSCF) wave functions constructed from gauge-including atomic orbitals (GIAOs). These magnetic criteria strongly suggest that, in contrast to the well-known aromaticity of the S 0 state of benzene, the T 1 and S 1 states of this molecule are antiaromatic. In square cyclobutadiene, which is shown to be considerably more antiaromatic than rectangular cyclobutadiene, the magnetic properties of the T 1 and S 1 states allow these to be classified as aromatic. According to the computed magnetic criteria, the T 1 state of rectangular cyclobutadiene is still aromatic, but the S 1 state is antiaromatic, just as the S 2 state of square cyclobutadiene; the S 2 state of rectangular cyclobutadiene is nonaromatic. The results demonstrate that the well-known "triplet aromaticity" of cyclic conjugated hydrocarbons represents a particular case of a broader concept of excited-state aromaticity and antiaromaticity. It is shown that while electronic excitation may lead to increased nuclear shieldings in certain low-lying electronic states, in general its main effect can be expected to be nuclear deshielding, which can be substantial for heavier nuclei. 相似文献
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Wenbi Guan 《International journal of environmental analytical chemistry》2013,93(6):679-691
A QuEChERS (quick, easy, cheap, effective, rugged, and safe) method for the determination of benazolin-ethyl and quizalofop-p-ethyl in rape and soil by high-performance liquid chromatography-tandem mass spectrometry has been developed in this study. The residue and dissipation of benazolin-ethyl and quizalofop-p-ethyl in rape and soil were determined with the developed method. The half-lives of benazolin-ethyl in rape straw and soil were 3.7–5.1 days and 14.3–26.3 days, respectively. The half-lives of quizalofop-p-ethyl in rape straw and soil were 5.0-6.1 days and 0.3–9.7 days, respectively. The residue of benazolin-ethyl and quizalofop-p-ethyl in rapeseed and soil were below the detection limit (i.e., 0.5?mg?kg?1, the maximum residue level of European Union for quizalofop-p-ethyl). 相似文献
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The P-anilino-P-chalcogeno(imino)diazasilaphosphetidines [Me(2)Si(mu-N(t)Bu)(2)P=E(NHPh)] (E = O (3), S (4), Se (5), N-p-tolyl (6)) were synthesized by oxidizing the P-anilinodiazasilaphosphetidine [Me(2)Si(N(t)Bu)(2)P(NHPh)] (2) with cumene hydroperoxide, sulfur, selenium, and p-tolyl azide, respectively. The lithium salt of 4 reacted with thallium monochloride to produce ([Me(2)Si(mu-N(t)Bu)(2)P=S(NPh)-kappaN-kappaS]Tl)(7), which features a two-coordinate thallium atom. Treatment of 4-6 with AlMe(3) gave the monoligand dimethylaluminum complexes ([Me(2)Si(mu-N(t)Bu)(2)P=E(NPh)-kappaN-kappaE]AlMe(2)) (E = S (8), Se (9), N-p-tolyl (10)), respectively. In these complexes the aluminum atom is tetrahedrally coordinated by one chelating ligand and two methyl groups, as a single-crystal X-ray analysis of 8 showed. A 2 equiv amount of 4-6 reacted with diethylzinc to produce the homoleptic diligand complexes ([Me(2)Si(mu-N(t)Bu)(2)P=E(NPh)-kappaN-kappaE](2)Zn)(E = S (11), Se (12), N-p-tolyl (13)). A crystal-structure analysis of 11 revealed a linear tetraspirocycle with a tetrahedrally coordinated, central zinc atom. 相似文献
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多环芳二酐型聚酯亚胺膜的透气性能李悦生,丁孟贤,徐纪平(浙江大学高分子科学与工程研究所,杭州,310027)(中国科学院长春应用化学研究所)关键词聚醚酰亚胺,聚酯酰亚胺,膜,透气性通常的聚酰亚胺加工性能较差,在芳环二酐的苯环间引入醚键等柔性基团后,其... 相似文献