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Mahmoud A. Abbady Hussein S. El-Kahef Mohamed A. Abd-Alla Maymouna M. Kandeel 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1984,34(2):62-72
Cyclonucleophilic addition of N-phthaloylaminoacid chlorides (II on 4-(N-ary-lideneamino)-4′-nitrodiphenyl sulphides (I) in dioxane and triethylamine afforded 4-(4″-aryl-3″-phthalylamino-2″-oxo-azetidin-1″-yl)-4′-nitro-diphenyl sulphides (III). Hydrazinolysis of III yielded 4-(4″-aryl-3″-amino-2″-oxo-azetidin-1″-yl)-4′-nitro-diphenyl sulphide hydrochlorides (IV). Condensation of IV with anisaldehyde using ethanol and piperidine as a basic catalyst gave 4-(4″-aryl-3″-anisylidine amino-2″-oxoazetidin-1″-yl)-4′-nitrodiphenylsulphides (V) in good yields. Interaction of V with chloroacetyl chloride in dioxane and triethylamine produced 4-(4″-aryl-3″-substituted β-lactamyl-2″-oxo-azetidin-1″-yi)-4′-nitrodiphenyl sulphides VI. Oxidation of IV, V and VI using hydrogen peroxide/glacial acetic acid mixtures gave the corresponding sulphones (VII), (VIII) and (IX). Sulphones of the type IX were obtained by unequivocal synthesis through interaction of sulphone-anils VIII with chloroacetyl chloride. The antibacterial activities of some of these compounds were determined. 相似文献
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Maher F. El-Zohry Abd El-Hamed N. Ahmed Farghaly A. Omar Mohamed A. Abd-Alla 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1992,53(4):329-336
Some aryl and/or heterocyclic mercaptans were allowed to react with 8-quinolyl chloroacetate (II), 8-quinolinoxyacetyl chloride (IV) and 3-(2′-chloroethyl)-2-methyl-3,4-dihydroquinazolin-4-one (X) in dry benzene and/or sodium hydroxide in absolute ethanol to give corresponding 8-quinolyl-α-mercaptoacetate (V), 8-quinolinoxythioacetate (VI) and 3-(2′-arylmercaptoethyl)-2-methyl-4-(3H)quinazolin-4-ones or 3-(2′-heterocyclicmercaptoethyl)-2-methyl-4(3H)-quinazolin-4-ones (XIa-h). The mercaptans V and XI were subjected to oxidation with hydrogen peroxide/acetic acid mixture (1:2) to afford the corresponding sulfones VII and XII. The structures of the synthesized compounds were elucidated by spectroscopic (IR and 1H-NMR) and elemental analyses. Some of these compounds were tested for their antimicrobial activities in comparison with tetracycline as a reference compound. 相似文献
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以1-金刚烷甲酸为原料,通过酯化、肼解制得1-金刚烷甲酰肼,1-金刚烷甲酰肼再与芳香醛反应得到相应的酰腙,最后以苯和DMF为溶剂,酰腙与巯基乙酸脱水环化成2-芳基-3-(1-金刚烷甲酰胺基)-4-噻唑啉酮类化合物,并利用IR、1HNMR、13CNMR、ESI-MS和元素分析对7个目标化合物的结构进行了表征。用MTT方法评价了它们在体外对HepG-2,A549-1和231-2 3种癌细胞株的体外生长抑制活性。结果表明,所合成的7个新化合物均具有潜在的体外抑制癌细胞生长活性。 相似文献
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合成了一系列新的5-取代苯氨基-6-叔丁基-1,2,4-三嗪-3-硫酮化合物,其结构经元素分析、IR、^1HNMR及MS等确证。实验发现目标化合物可以“一锅法”合成,产率较分步反应有较大提高。 相似文献
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利用二茂铁甲醛分别与1,2-乙二胺、1,3-丙二胺和1,4-丁二胺缩合,合成了3种双二茂铁基希夫碱,进行了生物活性实验。结果表明,3种双二茂铁基希夫碱对大肠埃希氏菌和金黄色葡萄球菌均具有较好的抗菌活性,1,3-丙二胺双缩二茂铁甲醛对金黄色葡萄球菌的抑菌能力最强,生物效价为210 U/mg(与四环素盐酸盐相比较);1,4-丁二胺双缩二茂铁甲醛对大肠埃希氏菌的抑菌能力最好,生物效价为1 058 U/mg(与四环素盐酸盐相比较)。3种双二茂铁基希夫碱对大肠埃希氏菌的抑菌能力比对金黄色葡萄球菌的抑菌能力强。 相似文献
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以2,4-二氯-5-氟苯乙酮为起始原料,通过β-酮酸酯化,与原甲酸三乙酯缩合,同2-氨基吡啶发生取代,再经环合反应、硼配合反应和哌嗪化反应合成得到了N-吡啶取代喹诺酮抗菌化合物,总收率为39.3%,并对其抗菌活性进行了试验。 相似文献
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Metal salts of mono(hydroxypentyl)phthalate [M(HPP)2, where M is Ca2+, Cd2+, Pb2+, or Zn2+] were synthesized by the reaction of 1,5‐pentane diol, phthalic anhydride, and metal acetate. A new series of metal‐containing polyurethanes containing ionic links in the main chain were synthesized by the reaction of hexamethylene diisocyanate or toluylene 2,4‐diisocyanate with the M(HPP)2 salts. The structures of the monomers and polymers were confirmed with infrared, 1H‐NMR, and 13C‐NMR spectra and elemental analysis. The polymers were also characterized with thermogravimetric analysis, differential scanning calorimetry, and solubility and viscosity measurements. The antibacterial activity of these polyurethanes was investigated with the agar diffusion method. © 2002 Wiley Periodicals, Inc. J Appl Polym Sci 85: 1194–1206, 2002 相似文献
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Two novel organotin monomers, (N‐tri‐n‐butyltin) maleimide and m‐acryloylamino‐(tri‐n‐butyltin benzoate), were synthesized. Copolymerization of these two monomers with styrene was carried out in the bulk at 65°C using asobisisobutyronitrile as the free radical initiator. The monomers and copolymers were characterized by elemental analysis; the molecular weights of the copolymers were determined by GPC, solubility, IR, and 1H‐NMR spectral studies. The antibacterial activities of the synthesized organotin monomers and copolymers toward various types of bacteria were also reported. © 2000 John Wiley & Sons, Inc. J Appl Polym Sci 77: 740–745, 2000 相似文献
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根据α,β-不饱和醛酮亲核加成反应原理合成化合物L{[3-(4-N,N-dimethyl-pyenyl)-5-Anthracen-9-yl]-Pyrazoline}和化合物M[3-ferroceny-5-(Anthracen-9-yl)-Pyrazoline]。利用~1H NMR和~(13)C NMR对化合物进行结构表征,通过抑菌实验研究化合物抑菌生物活性。探析新型吡唑啉衍生物对革兰氏阳性菌、革兰氏阴性菌和真菌的抑菌效果,研究其结构变化对活性的影响。结果表明,化合物L和M对典型革兰氏阳性菌和典型革兰氏阴性菌有一定的抑菌效果,对真核细胞型微生物作用不明显。通过比较两者对细菌的作用结果(抑菌圈直径的大小),化合物L的抑菌作用明显强于化合物M,化合物L吡唑啉环连接N、N-二甲基苯环可能增强了抑菌生物活性。 相似文献
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壳聚糖与柠檬醛缩合反应产席夫碱及其抗菌活性 总被引:2,自引:0,他引:2
通过壳聚糖与柠檬醛在超声波振荡下反应制备了壳聚糖缩柠檬醛席夫碱。采用[L9(33)]正交实验探讨了反应时间、反应温度及反应物配比对壳聚糖席夫碱缩合率和取代度的影响。最佳条件为:反应物配比n(壳聚糖)∶n(柠檬醛)=1∶6,反应温度40~50 ℃,反应时间10 h,壳聚糖席夫碱的缩合率可达86%,取代度为0.82。红外光谱和X射线衍射光谱结果表明产物具有壳聚糖席夫碱的结构特征。对大肠杆菌、金黄色葡萄球菌和黑曲霉的抗菌实验表明,该产物对大肠杆菌、金黄色葡萄球菌和黑曲霉的最低抑菌浓度分别为1 g/L、1 g/L和5 g/L,其抗菌活性随浓度的增加而增加,且优于壳聚糖。 相似文献
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Amphoteric terpolymers of acrylic acid (AA), acrylamide (AM), and N,N′‐dimethyl‐N‐ethylmeth‐acryloxylethylammoniumbromide (DMAEA‐EB) with varied compositions P[AA‐AM‐(DMAEA‐EB)] were synthesized by inverse suspension polymerization. The components of P[AA‐AM‐(DMAEA‐EB)] were verified by FTIR spectroscopy. The water absorption ability and antibacterial activity of the copolymer against Escherichia coli(E. coli) and Staphylococcus hyicus(S. hyicus) suspended in sterilized physiological saline were investigated. The introduction of N+R4 may increase the water absorbency of P[AA‐AM‐(DMAEA‐EB)] in some degree because of the excellent hydrophilicity of N+R4. The AA‐AM‐(DMAEA‐EB) hydrogels exhibited high antibacterial activity against bacteria tested. The process of adsorption between live bacteria cells and resins was at least partially reversible. A peak of antibacterial efficiency existed with increasing contact time. The resin killed 96.6% E. coli organisms and 90.3% S. hyicus organisms, respectively, within 30 min of contact at dosage of 0.1g. The concentration of DMAEA‐EB has a special effect on the antibacterial activity of the polyampholytic hydrogels, which is different from polycation. It was observed that the antibacterial activity of the resin with 2 mol % of DMAEA‐EB is superior to the copolymers tested with other compositions. © 2009 Wiley Periodicals, Inc. J Appl Polym Sci, 2009 相似文献
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采用化学还原法,以硝酸银(AgNO3)、过氧化氢(H2O2)和聚乙烯吡咯烷酮(PVP)等为原料制备了纳米银粉无机抗菌剂,然后将其加入到聚丙烯酸酯粘合剂体系中制备纳米银粉抗菌整理液,并通过抑菌圈法对其抗菌性能进行了评价。实验结果表明,纳米银粉抗菌剂较佳的反应条件为w(AgNO3溶液)=5%,活化时间为12h,w(H2O2溶液)=6%,w(PVP溶液)=5%,反应温度为40℃,反应时间为3h;当抗菌整理液中银粉浓度为0.5g/L时,对金黄色葡萄球菌的抑菌圈直径为13.1mm,对大肠杆菌的抑菌圈直径为13.7mm。将抗菌试验后的试样放置6个月后,抑菌环仍然清晰未受细菌感染;该纳米银粉无机抗菌剂具有优良的抗菌性能和抗菌持久性。 相似文献
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报道了配合物GdI3.2CS(NH2)2.10H2O的新合成方法,通过元素分析、X-射线粉末衍射、红外光谱、质谱、差热-热重分析,确定了配合物的组成和结构,首次测定了配体碘化钆、硫脲和配合物对枯草芽孢杆菌、葡萄球菌和大肠杆菌的抗菌活性。抗菌活性测试结果表明,所有试样对枯草芽孢杆菌的杀死作用显著,且高浓度溶液(0.05 mol/L)比低浓度溶液(0.01 mol/L)的抗菌效果好;对金黄色葡萄球菌、大肠杆菌的杀死作用不明显;浓度为0.05 mol/L时,配合物GdI3.2CS(NH2)2.10H2O对枯草芽孢杆菌的杀死作用大于CS(NH2)2和GdI3.9H2O。 相似文献
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S. R. El-ezbawy M. A. Alshaikh 《Journal of chemical technology and biotechnology (Oxford, Oxfordshire : 1986)》1990,47(3):209-218
10-(Hetero/arylthio)acetyl-2-chlorophenothiazines II have been synthesized via interaction of 10-chloroacetyl-2-chlorophenothiazine I with heterocyclic and/or aromatic potassium mercaptide in ethanol. Oxidation of II using H2O2/CH3COOH mixture was studied. Structures of the products were verified by elemental and spectral analyses. Some compounds were screened in vitro for their antibacterial activities. 相似文献
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稀土-蛋氨酸-邻菲咯啉配合物的合成、表征及抗菌活性研究 总被引:2,自引:1,他引:2
采用冷凝回流法合成了4种新型稀土(镧、铕、钐和钕)-蛋氨酸-邻菲咯啉三元配合物,通过元素分析、EDTA-滴定、摩尔电导、红外光谱,确定了配合物的组成为RE(Met)_3phenCl_3·3H_2O(RE:La~(3+)、Eu~(3+)、Sm~(3+)、Nd~(3+);Met=L-蛋氨酸;phen=邻菲咯啉).抗菌活性的研究表明,与配体相比,稀土三元配合物对大肠杆菌(Escherichia coli)和金黄色葡萄球菌(Staphylococcus aureus)均具有更强的抑菌能力. 相似文献