共查询到19条相似文献,搜索用时 155 毫秒
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2-乙酰噻吩吖嗪及其过渡金属配合物的合成与活性 总被引:1,自引:0,他引:1
目的 研究2-乙酰噻吩吖嗪及其过渡金属Cu^2 ,Fe^3 配合物的合成与生物活性。方法 从2-乙酰噻吩和水合肼出发合成2-乙酰噻吩吖嗪,进而合成了其过渡金属Cu^2 ,Fe^3 的配合物。用MS,^1H—NMR对配体进行了确认。通过元素分析、摩尔电导率、红外光谱、紫外光谱等手段对配合物进行了表征。用NBT法研究了配合物对超氧阴离子自由基的抑制作用;并利用MTT法和SRB法对其进行了抗肿瘤活性体外筛选实验。结果 发现配体和配合物都具有一定的生物活性,且Cu配合物活性较好。结论 配合物的生物活性可能与中心离子的最外层d轨道的电子结构有关。 相似文献
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目的:合成大黄酸的三种金属配合物并对其结构进行表征,对比研究配体和配合物对三种细菌的体外抑菌活性大小。方法:在无水乙醇中合成了大黄酸的三种金属配合物,采用紫外光谱法,红外光谱法,核磁共振氢谱法对产物结构进行表征,确定了配合物的组成及结构。采用二倍稀释法测定了配合物的最小抑菌浓度(MIC),采用滤纸片法测定了配体及配合物对金黄色葡萄球菌、肺炎链球菌、大肠杆菌的抑菌活性大小。结果:合成的配合物经结构表征后,初步确定了其可能结构式为2分子大黄酸和1分子金属离子配位,抑菌活性测试结果表明,配合物的抑菌活性强于配体,其中大黄酸锰对于金黄色葡萄球菌以及大肠杆菌抑制作用都最强,抑菌圈大小分别达到了23.3、20.5 mm;而大黄酸钴对肺炎链球菌抑菌活性最强,抑菌圈达22.5 mm。二倍稀释法得出了配合物和配体的MIC值(最小抑菌浓度),根据该值大小可知,配合物抑菌活性总体上强于配体,但也有少部分与配体相当。结论:大黄酸和金属离子形成配合物后,抑菌活性增强。 相似文献
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Cefadroxil drug loaded biopolymeric films of chitosan-furfural schiff base were prepared by reacting chitosan with furfural in presence of acetic acid and perchloric acid respectively for the external use. Prepared films were evaluated for their strength, swelling index, thickness, drug content, uniformity, tensile strength, percent elongation, FTIR spectral analysis and SEM. The results of in vitro diffusion studies revealed that the films exhibited enhanced drug diffusion as compared to the films prepared using untreated chitosan. The films also demonstrated good to moderate antibacterial activities against selective gram positive and gram negative bacteria. 相似文献
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N. M. Goudgaon N. J. Basha S. B. Patil 《Indian journal of pharmaceutical sciences》2009,71(6):672-677
4-Substituted-5-iodo-2-benzylthiopyrimidines were prepared efficiently in three steps. 2-Benzylthiopyrimidine on iodination in presence of base gave 5-iodo-2-benzylthiopyrimidine (1), which on chlorination with excess of POCl3 furnished 4-chloro-5-iodo-2-benzylthiopyrimidine (2). Reaction of 2 with substituted aromatic amines, 2-aminopyridine and hydrazine hydrate yielded 4-amino-5-iodo-2-benzylthiopyrimidines 3(a-e), (3f) and (3g) respectively. Further, 4-hydrazino-5-iodo-2-benzylthiopyrimidine on condensation with substituted aromatic and heterocyclic aldehydes afforded the corresponding schiff bases 4(a-h). The structure of synthesized compounds have been established by spectral studies and elemental analysis. Synthesized compounds have been screened for antimicrobial activity. Compound 3f exhibited good antifungal activity against A. niger. The compounds 4a, 4c, 4d, 4g and 4h exhibited good antibacterial activity. 相似文献
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Some new schiff bases (1a-d) 4-thiazolidinones (2a-d) have been synthesised and tested for their antibacterial activity. The structures of these compounds have been established on the basis of elemental analysis and spectral data (IR and H1 NMR). 相似文献
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目的:寻找具有更好抗菌活性的含硫三环氟喹诺酮类化合物。方法:在芦氟沙星母核的10位引入不同基团,设计并合成8个含硫三环氟喹诺酮类化合物,并测定其体外抗菌活性。结果:合成了目标化合物,其结构经IR、^1HNMR、MS和元素分析确证;它们具有不同强度的抗菌活性,其中几个化合物的抗菌活性优于芦氟沙星。结论:初步的体外抗菌实验证实所合成目标化合物具明显的抗菌活性,甚至优于芦氟沙星。 相似文献
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New broad-spectrum alkylthio cephalosporins 总被引:1,自引:0,他引:1
G Nannini G Molgora G Biasoli P Cozzi F Casabuona G Galli D Severino L Sala C Confalonieri P N Giraldi G Vita I de Carneri G Meinardi G Monti A Bianchi 《Arzneimittel-Forschung》1977,27(2):343-352
A series of 7-substituted alkyl-thio-acylaminocephalosporins with the following general formula were prepared and tested for in vitro antibacterial activity: (formula: see text). We tried in our research to find any relationship between antibacterial activity and pharmacokinetic properties on the one hand, and chemical structure on the other. The most interesting products were also studied for their in vivo antibacterial activity in experimental acute systemic infections in the mouse. 相似文献
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A series of novel Schiff base tetradentate ligands and its iron (III) coordination compounds were synthesized, characterized and evaluated for antibacterial and antioxidant activity. All the synthesized ligands and complexes were characterized by spectroscopic and crystallographic techniques. Electronic spectra, Mössbauer spectra, magnetic moment and conductance study evidence the fact of octahedral arrangement around iron (III). The in vitro antimicrobial Schiff base complexes bear polar and nonpolar properties together; this makes them suitable for permeation to the cells and tissues, it enhances the activity against the bacteria. The antioxidant properties were measured with DPPH (2,2’-diphenyl-2-picrylhydrazyl). These properties were due to the unique feature of ligands such as highest lipophilicity, lowest electron withdrawing power and highest polarisability. 相似文献
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This review paper has attempted information specific to the title compound. This survey of the literature data provides useful information about the design and stabilities of the triorganotin with biologically active ligands. Up to now, considerable efforts have been made to synthesize and characterize triorganotin(IV) schiff base complexes with the general formulae R3ML [R = organic group, M: Sn and L: schiff base] and many studies have been focused in order to understand bioassay results. Users with an interest in this substance are strongly encouraged for future research that this is still a very open field. 相似文献
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C H Park D R Brittelli C L Wang F D Marsh W A Gregory M A Wuonola R J McRipley V S Eberly A M Slee M Forbes 《Journal of medicinal chemistry》1992,35(6):1156-1165
The synthesis and structure-activity relationship (SAR) studies of the effect of different polysubstitution patterns in the aromatic ring of 5-(acetamidomethyl)oxazolidinone antibacterials (I) on antibacterial activity are presented. Compounds I were prepared by the six-step synthesis described previously (Gregory, W. A.; et al. J. Med. Chem. [formula: see text] 1989, 32, 1673), electrophilic aromatic substitution reactions of 3-substituted compounds, and functional-group interchange reactions of 3,4-disubstituted compounds. Antibacterial evaluation of compounds I against Staphylococcus aureus and Enterococcus faecalis gave the following results. The 2,4- and 2,5-disubstituted derivatives have weak or no antibacterial activity. Antibacterial activities of 3,4-disubstituted compounds are comparable to those of the 4-monosubstituted analogues for small 3-substituents (smaller than Br), but decline rapidly for larger 3-substituents. 3,4-Annulated derivatives are comparable in activity to their open-chain analogues. 3,5-Disubstituted and 3,4,5- and 2,4,6-trisubstituted derivatives are devoid of antibacterial activity. 相似文献