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2'-羟基查耳酮的Mannich反应及其产物的生物活性 总被引:2,自引:0,他引:2
研究了2'-羟基查耳酮的Mannich反应, 发现该反应区域选择性地发生在查耳酮B环C-3'位, 利用此法共合成了12个新的Mannich碱化合物, 其结构经元素分析、1H NMR和IR得到确证. 该反应制备步骤简单, 条件温和, 产物易纯化, 收率从中等到高(49~72%). 初步的生物活性测定表明其中部分化合物具强效的CDK1/cyclin B抑制活性, 多数化合物对肿瘤细胞具较强的抑制活性. 相似文献
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本文综述了用酮作为酸性组分合成Mannich碱的最近进展。内容包括:β-脂氨基酮、β-芳氨基酮的合成和分子内Mannich反应。 相似文献
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含硫Schiff碱的合成及其抑菌活性 总被引:2,自引:0,他引:2
1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮分别与氨基硫脲、肼基二硫代甲酸苄酯、肼基二硫代甲酸甲酯和1,3-二氨基硫脲反应合成了6个含硫Schiff碱(6a~6 e),其结构经UV,1H NMR,IR和元素分析表征。初步生物活性测试结果表明,部分6对大肠杆菌和枯草芽孢杆菌具有一定的抑菌活性。 相似文献
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以(取代)水杨醛、间(对)羧基苯胺和氨基甲酰肼为原料,分别采用冰浴法合成了4-(二乙基氨基)水杨醛-3-羧基苯胺(3a),4-(二乙基氨基)水杨醛-4-羧基苯胺(3b)和水杨醛-3-羧基苯胺(3c);采用固相法合成了4-(二乙基氨基)水杨醛-氨基甲酰肼(3d);采用水浴回流法合成了3,5-二溴水杨醛-4-羧基苯胺(3e)和2-羟基-1-萘甲醛-4-羧基苯胺(3f),3a~3f均为新化合物,其结构经1H NMR,IR,ESI-MS和元素分析表征。研究了3a~3f对大肠杆菌、金黄色葡萄球菌及欧文氏草生杆菌的抑菌活性。结果表明:3a~3f对受试菌种均有一定的抑菌活性,其中3e的抑菌活性最好。 相似文献
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以邻苯二胺和香草醛为原料,合成了3个新型的香草醛缩苯并咪唑Schiff碱(5a~5c),其结构经1H NMR和IR表征。用菌丝生长速率法研究了5a~5c对小麦赤霉病菌(F.gra),马铃薯干腐病菌(F.oxy),玉米弯苞叶斑病菌(C.sor),番茄早疫病菌(A.sol)和棉花枯萎病菌(F.oxy.s.v)的抑制活性。结果表明:香草醛缩2-甲基-5-氨基苯并咪唑(5c)对F.gra, F.oxy和C.sor的抑制活性高于多菌灵,其EC50值分别为19.76 mg·L-1, 24.94 mg·L-1和29.15 mg·L-1。 相似文献
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芳香酮与芳香醛及芳香胺的Mannich反应 总被引:6,自引:0,他引:6
醛、酮与芳香醛及芳香胺的 Mannich 反应,文献[1]曾报道在 HCl-EtOH 溶液中苯乙酮及甲醛与芳香胺的 Mannich 反应。本文在此基 相似文献
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以壳聚糖(CTS)、水杨醛(Sal)、2-羟基-4-甲氧基苯甲醛(2-Hy)、香草醛(Val)和邻香草醛(O-val)为原料,经过缩合反应得到四种壳聚糖衍生物(CTS-Sal,CTS-2Hy,CTS-Val,CTS-O-val),采用红外光谱(FT-IR)和紫外分光光谱(UV)对结构进行了表征。通过微量液体稀释法和真菌菌丝生长速率法测定了四种衍生物对灰霉菌的最小抑菌浓度(MIC)和半抑制量浓度(EC50)。结果表明,与CTS相比,四种衍生物对灰霉菌均有明显抑制作用,其中CTS-2Hy的MIC和EC50均最小,分别为1 184.49μg·m L-1和724.44μg·m L-1。 相似文献
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以易制备的无保护NH-亚砜亚胺和廉价易得的取代甲苯为原料,利用可见光催化策略,在较为温和的条件下实现了NH-亚砜亚胺和取代甲苯的偶联反应。考察了不同光催化剂、碱和溶剂等因素对反应的影响,筛选出了最优的反应条件,拓展了亚砜亚胺和甲苯的底物范围,并对产物的抑菌活性进行了初步研究。结果表明,反应最佳条件为:亚砜亚胺(0.2 mmol),甲苯(0.24 mmol),碳酸钾(0.26 mmol),曙红Y(0.02 mmol),NBS (0.26 mmol),异丙醇(1 mL),在18 W蓝光LED光照下,室温反应24 h。该反应体系对不同的亚砜亚胺底物和甲苯底物均有良好的适用性,产率在46%~75%。在16个被试化合物中,有7个化合物对大肠杆菌有抑制作用,6个化合物对金黄色葡萄球菌有抑制作用。 相似文献
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5-烃基丙二酸亚异丙酯的Mannich碱和甲基酮在弱酸如醋酸的存在下, 合成得到缩合产物5-(3-氧代烃基)丙二酸亚异丙酯(3). 相似文献
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《Arabian Journal of Chemistry》2014,7(6):994-999
A series of 2-(phenyl)-2-(morpholin-4-yl)-N-phenylacetamide I–VII were synthesized by Mannich base method. Synthesized compounds I–VII were confirmed by IR, 1H NMR, 13C NMR, mass and elemental analyses. Synthesized compounds I–VII were screened for antibacterial activity against various bacterial strains and compared with standard Ciprofloxacin at concentration 100 μg/mL and for antifungal activity against various fungal strains and compared with Clotrimazole at concentration 100 μg/mL; particularly 3-(4-chlorophenyl)-3-(morp holin-4-yl)-N-phenylpropanamide lll that has high antibacterial activity against Streptococcus epidermidis was compared with standard Ciprofloxacin. 相似文献
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With the aim of developing potential antimicrobials, a series of novel Ciprofloxacin methylene isatin derivatives incorporating different aromatic aldehydes were synthesized and characterized by FTIR, 1H NMR, Mass spectroscopy and bases of elemental analysis. In addition, the in vitro antibacterial and antifungal properties were tested against some human pathogenic microorganisms by employing the disc diffusion technique. A majority of compounds were showing activity against several of the microorganisms. The relationship between the functional group variation and the biological activity of the evaluated compounds is discussed. From comparisons of the compounds, 3c was determined to be the most active compound. 相似文献
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Jiao Wang~a Ying Zhong~ 《中国化学快报》2008,19(4):387-389
Five new C-8 Mannich base derivatives of irisolidone 2a-2e were synthesized and their nitric oxide(NO)production inhibitory activity was evaluated.Compounds 2a,2b,2c and 2e displayed stronger activities in vitro than the parent compound irisolidone. 相似文献
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Jakub Iwanejko Elżbieta Wojaczyńska Justyna Trynda Magdalena Maciejewska Joanna Wietrzyk Andrzej Kochel Jacek Wojaczyński 《Tetrahedron》2017,73(16):2276-2282
Tests of antiproliferative activity of Mannich adducts of aromatic nucleophiles and a chiral bicyclic imine revealed a di-tert-butylphenol derivative as a promising compound for further exploration. To study the influence of substitution pattern and a configuration of stereogenic centers on the inhibition of cancer cell growth, a series of Mannich bases were obtained with a good to high diastereoselectivity from the reaction of the imine and three isomeric di-tert-butylphenols. Six new enantiopure adducts were isolated and fully characterized. Selected derivatives were shown to exhibit an interesting antiproliferative activity comparable to cisplatin. 相似文献
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The catalytic action of aqueous NaOH at 20 °C on 2,2,6,6-tetramethyl-3-(N-methyl-piperidiniomethyl)-4-oxopiperidine 1-oxyl iodide rapidly resulted in the formation (k = 57 L mol−1 s−1) of a paramagnetic ketone with an activated double bond: 2,2,6,6-tetramethyl-3-methylidene-4-oxopiperidine 1-oxyl. The latter
underwent slow transformation into a nitroxyl biradical containing an activated double bond and a methylene bridge linking
positions 3 and 3′.
Published in Russian in Izvestiya Akademii Nauk. Seriya Khimicheskaya, No. 2, pp. 421–423, February, 2008. 相似文献
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Alexander D. Dilman Vladimir V. Gorokhov Pavel A. Belyakov Marina I. Struchkova Vladimir A. Tartakovsky 《Tetrahedron letters》2006,47(35):6217-6219
The synthesis of α-C6F5-substituted amines by a three-component coupling reaction of C6F5SiF3, aromatic aldehydes, and N-trimethylsilylamines has been elaborated. The optimized conditions include performing the reaction in dimethylformamide in the presence of stoichiometric amounts of lithium acetate. 相似文献
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《Journal of Coordination Chemistry》2012,65(18):3256-3267
Dinuclear molybdenum(VI) peroxo complexes containing Mannich base ligands having formulae [Mo2O4(O2)2L-L(H2O)2] · H2O [where L-L = N-[1-morpholinobenzyl] acetamide (MBA), N-[1-piperidinobenzyl] acetamide (PBA), N-[1-morpholino(-4-nitrobenzyl)] benzamide (MPNBB), N-[1-piperidino(-3-nitrobenzyl)] benzamide (PMNBB), N-[1-morpholino(-2-nitrobenzyl)] acetamide (MONBA), and N-[1-morpholino(-3-nitrobenzyl)] acetamide (MMNBA)] have been synthesized by stirring ammonium heptamolybdate with excess 30% aqueous hydrogen peroxide followed by treatment with ethanolic solution of corresponding ligands. The complexes have been characterized by elemental analysis, molar conductance, magnetic measurements, infrared (IR), electronic, TGA/DTA, mass spectral, and 1H NMR studies. The complexes are non-electrolytes and diamagnetic. The IR spectral studies suggest that the ligands are bidentate to metal through carbonyl oxygen and ring nitrogen. Thermal analyses provide conclusive evidence for the presence of coordinated, as well as lattice water in the complexes. Dinuclear complexes preserve the individuality of the molybdenum oxo peroxo core. The complexes exhibit higher antibacterial activity against bacterium Ralastonia solanacearum (Pseudomonas solanacearum) than the free ligands. 相似文献