间氟苯乙醛缩乙醇胺席夫碱抑菌活性研究

目的试验新合成的化合物间氟苯乙醛缩乙醇胺席夫碱对枯草杆菌等五种细菌的抑菌作用,为寻找具有抑菌、抗癌、抗病毒、杀霉等生物活性的药物提供新药。方法采用国际药典通用的管碟法。首先培养枯草杆菌、大肠杆菌、大肠杆菌(101)、金黄色葡萄球菌、革兰阴性细菌(发荧光Q67)等五种细菌,取其第二代繁殖体作受试对象。将间氟苯乙醛缩乙醇胺席夫碱用适量蒸馏水溶解,配制浓度为0.25,0.5,1,2mg/mL一系列溶液,加样后除革兰阴性细菌(发荧光Q67)在25℃培养箱里培养24 h,其余均在室温下培养24 h,实验中以蒸馏水作为对照。结果作为对照的蒸馏水对上述细菌无任何抑制作用,该席夫碱对上述细菌均有不同程度的抑制作用。结论抑菌活性实验表明该席夫碱对枯草杆菌、大肠杆菌、大肠杆菌(101)、金黄色葡萄球菌、革兰阴性细菌(发荧光Q67)等五种细菌均有较好的抑菌作用。     

对氟苯乙醛缩乙醇胺席夫碱抑菌活性研究

目的　试验新合成的化合物对氟苯乙醛缩乙醇胺席夫碱(含氟席夫碱)对枯草杆菌等五种细菌的抑菌作用,为寻找具有抑菌、抗癌、抗病毒、杀霉等生物活性的药物提供新药。方法　采用国际药典通用的管碟法。首先培养枯草杆菌、大肠杆菌、大肠杆菌(101)、金黄色葡萄球菌、革兰阴性细菌(发荧光Q₆₇)等五种细菌,取其第二代繁殖体作受试对象。将对氟苯乙醛缩乙醇胺席夫碱用适量蒸馏水溶解,配制浓度为0.25,0.5,1,2mg/mL一系列溶液,加样后革兰阴性细菌(发荧光Q₆₇)在25℃培养箱里培养24h,其余均在室温下培养24h,实验中以蒸馏水作为对照。结果　蒸馏水对上述细菌无任何抑制作用,该含氟席夫碱对上述细菌均有不同程度的抑制作用。结论　抑菌活性实验表明该含氟席夫碱对枯草杆菌、大肠杆菌、大肠杆菌(101)、金黄色葡萄球菌、革兰氏阴性细菌(发荧光Q₆₇)等五种细菌均有较好的抑菌作用。     

间氟苯乙醛缩乙醇胺席夫碱抑菌活性研究

目的试验新合成的化合物间氟苯乙醛缩乙醇胺席夫碱对枯草杆菌等五种细菌的抑菌作用,为寻找具有抑菌、抗癌、抗病毒、杀霉等生物活性的药物提供新药。方法采用国际药典通用的管碟法。首先培养枯草杆菌、大肠杆菌、大肠杆菌(101)、金黄色葡萄球菌、革兰阴性细菌(发荧光Q₆₇)等五种细菌,取其第二代繁殖体作受试对象。将间氟苯乙醛缩乙醇胺席夫碱用适量蒸馏水溶解,配制浓度为0.25,0.5,1,2mg/mL一系列溶液,加样后除革兰阴性细菌(发荧光Q₆₇)在25℃培养箱里培养24 h,其余均在室温下培养24 h,实验中以蒸馏水作为对照。结果作为对照的蒸馏水对上述细菌无任何抑制作用,该席夫碱对上述细菌均有不同程度的抑制作用。结论抑菌活性实验表明该席夫碱对枯草杆菌、大肠杆菌、大肠杆菌(101)、金黄色葡萄球菌、革兰阴性细菌(发荧光Q₆₇)等五种细菌均有较好的抑菌作用。     

香草醛缩乙醇胺席夫碱的合成、表征与抑菌活性研究

目的与方法合成了未经报道的香草醛缩乙醇胺席夫碱,并对其进行了结构表征.结果与结论初步确认了其组成,抑菌实验表明该席夫碱对枯草杆菌、大肠杆菌、金黄色葡萄球菌、革兰氏阴性细菌(发荧光Q67)均有较好的抑制作用.     

3,4-二甲氧基苯甲醛缩乙醇胺席夫碱合成、表征与抑菌活性研究

目的与方法合成了未经报道的3,4-二甲氧基苯甲醛缩乙醇胺席夫碱,并对其进行了结构表征。结果与结论初步确认了其组成,抑菌实验表明该席夫碱对枯草杆菌、大肠杆菌、金黄色葡萄球菌、革兰氏阴性细菌(发荧光Q67)均有较好的抑制作用。     

香草醛缩乙醇胺席夫碱的合成、表征与抑菌活性研究

目的与方法　合成了未经报道的香草醛缩乙醇胺席夫碱,并对其进行了结构表征。结果与结论　初步确认了其组成,抑菌实验表明该席夫碱对枯草杆菌、大肠杆菌、金黄色葡萄球菌、革兰氏阴性细菌(发荧光Q₆₇)均有较好的抑制作用。     

3,4-二甲氧基苯甲醛缩乙醇胺席夫碱合成、表征与抑菌活性研究

目的与方法合成了未经报道的3,4-二甲氧基苯甲醛缩乙醇胺席夫碱,并对其进行了结构表征。结果与结论初步确认了其组成,抑菌实验表明该席夫碱对枯草杆菌、大肠杆菌、金黄色葡萄球菌、革兰氏阴性细菌(发荧光Q₆₇)均有较好的抑制作用。     

二十五味鬼臼丸体外的抑菌作用

目的 考察藏药二十五味鬼臼丸的体外抑菌作用.方法 采用M-H琼脂平板、PDA琼脂平板和微量稀释法检测藏药二十五味鬼臼丸对金黄色葡萄球菌ATCC25923、大肠杆菌ATCC25922、铜绿假单胞菌ATCC27853,枯草杆菌、耐药表皮葡萄球菌、白色念珠球菌、非耐药金黄色葡萄球菌、腊状芽孢杆菌、粪肠球菌的抑菌圈和最小抑菌浓度(MIC).结果 对耐药表皮葡萄球菌等9种常见革兰阳性和阴性菌都有明显的体外抑菌作用;不同溶剂药液的抑菌活性具有明显差异.结论 二十五味鬼臼丸对临床分离菌株白色念珠球菌和耐药表皮葡萄球菌有较强的抑制作用,具有较高的临床应用价值.     

中药"铁扇癣痒平"体外抑菌试验

目的观察"铁扇癣痒平"体外抗菌效果和抑菌浓度.方法采用对倍液体稀释法测定该药对金黄色葡萄球菌、大肠杆菌、红色毛癣菌、紫色毛癣菌、须毛癣菌和石膏样小孢子菌体外抑制作用.以市售的复方土槿皮酊、庆大霉素和二性霉素B为对照.结果体外抑菌试验结果表明,该药对细菌(金黄色葡萄球菌、大肠杆菌)和真菌(红色毛癣菌、紫色毛癣菌、须毛癣菌、石膏样小孢子菌)均有抑制作用.结论"铁扇癣痒平"具有体外抑制革兰阳性、革兰阴性细菌和皮肤真菌的作用,且抗真菌活性高于抗细菌活性.     

余甘子4种不同部位醇提物的抑菌作用研究

目的:研究余甘子4种提取物的抑菌作用。方法:对余甘子醇提物通过抑菌环法测定抑菌活性,对作用明显的菌种进行部位活性测试,对活性部位采用二倍稀释法测定最低抑菌浓度。结果:余甘子醇提物对金黄色葡萄球菌、枯草杆菌、大肠杆菌和白色念珠菌有强抑制作用,对绿脓杆菌、产气夹膜杆菌、青霉、啤酒酵母和黑曲霉有抑制作用;余甘子醇提物石油醚部位和乙酸乙酯部位对金黄色葡萄球菌、枯草杆菌、大肠杆菌和白色念珠菌有强抑制作用,乙酸乙酯部位对金黄色葡萄球菌,枯草杆菌,大肠杆菌和白色念珠菌的最低抑制浓度分别为0.0625、0.125、0.0625、0.25mg·mL-1。结论:余甘子醇提物有较强的抑菌作用,乙酸乙酯部位为其抑菌活性部位。     

头孢地嗪钠体内、外抗菌活性研究

目的:评价国产及进口头孢地嗪钠(CDZ)体内、外抗菌活性。方法:采用琼脂平皿稀释法及试管稀释法测定国产CDZ及其进口制剂、头孢氨噻肟钠对300株临床分离致病菌的最低抑菌浓度( MIC) ;采用小鼠腹腔感染模型,观察CDZ对大肠杆菌、克雷伯氏肺炎杆菌及金黄色葡萄球菌感染小鼠的体内抗菌作用,按Bliss法计算半数有效剂量(ED50)值。结果:国产和进口CDZ对大部分革兰阴性菌,革兰阳性菌中的肺炎球菌、乙型链球菌等具有显著的抗菌活性,MIC90大多为0.012～1.0μg·mL-1。对阴沟杆菌、产气杆菌和沙雷氏菌具有中度抗菌活性,对甲氧西林敏感金黄色葡萄球菌、表皮葡萄球菌抗菌活性较差,MIC50为4μg·mL-1。对本实验所试绿脓杆菌、不动杆菌、肠球菌、甲氧西林耐药金黄色葡萄球菌耐药。对敏感大肠杆菌、克雷伯氏肺炎杆菌及金黄色葡萄球菌感染模型小鼠均具有较好保护作用,两者疗效相近。结论:国产与进口CDZ具有较强和相同的抗菌活性。     

DNA cleavage and antimicrobial investigation of Co(II), Ni(II), and Cu(II) complexes with triazole Schiff bases: synthesis and spectral characterization

The Co(II), Ni(II), and Cu(II) complexes with Schiff bases derived from 3-substituted-4-amino-5-mercapto-1,2,4-triazole and fluvastatin have been synthesized. Schiff bases exhibited thiol–thione tautomerism and coordinated to metal ion through azomethine nitrogen and thiolate sulphur atoms. Square planar geometry for all the metal complexes of the type ML₂ has been proposed in the light of analytical, spectral (IR, UV–Vis., ESR, and FAB-mass), magnetic, and thermal studies. The antimicrobial studies of Schiff bases and their metal complexes against various antibacterial (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa and Bacillus subtilis) and antifungal (Aspergillus niger, and Pencillium Chrysogenum) species by Minimum Inhibitory Concentration method revealed that, the metal complexes possess more healing antibacterial activity than the Schiff bases. Co(II), Ni(II), and Cu(II) complexes cleave the DNA isolated from A. niger.     

In vitro antibacterial, antifungal, and DNA cleavage studies of coumarin Schiff bases and their metal complexes: synthesis and spectral characterization

A series of metal complexes of the type ML·2H₂O [M?=?Co(II), Ni(II), and Cu(II)] have been synthesized with newly synthesized Schiff bases derived from 1,8-diaminonaphthalene and 8-formyl-7-hydroxy-4-methylcoumarin/8-acetyl-7-hydroxy-4-methylcoumarin. The chelation of the metal complexes has been proposed in the light of analytical, spectral (IR, NMR, UV–Vis, ESR, and FAB-mass), magnetic, and thermal studies. The redox behavior of the complexes was investigated by electrochemical method using cyclic voltammetry. The Schiff bases and their complexes have been screened for their antibacterial (Escherichia coli, Staphylococcus aureus, Pseudomonas aeruginosa, and Salmonella typhi) and antifungal activities (Aspergillus niger, Aspergillus flavus, and Cladosporium) by minimum inhibitory concentration method. The results of these studies show the metal complexes to be more effective antibacterial and antifungal as compared with the uncomplexed coumarins. DNA cleavage is studied by agarose gel electrophoresis method.     

Antibacterial and antifungal oxovanadium(IV) complexes of triazole-derived Schiff bases

A newly synthesised series of antibacterial and antifungal triazole-derived Schiff base ligands (L ¹ )–(L ⁵ ) has been prepared by the condensation reaction of 3,5-diamino-1,2,4-triazole with methyl-, chloro- and nitro-substituted thiophene-2-carboxaldehydes in (1:2) molar ratio. The most probable structures of the synthesised Schiff base ligands were established on the basis of their physical, spectral (IR, ¹H and ¹³C NMR and mass spectrometry) and analytical (CHN analysis) data. These Schiff bases potentially act as bidentate ligand and were further made to react with the vanadyl(IV) sulphate (VOSO₄·5H₂O) in (1:2) (metal:ligand) molar ratio to prepare their oxovanadium(IV) complexes (1)–(5). All oxovanadium(IV) complexes showed a square-pyramidal geometry which was established on the basis of their physical, spectral and analytical data. The Schiff base ligands and their vanadyl(IV) complexes have been screened for their in vitro antibacterial, antifungal and brine shrimp bioassay. The antimicrobial activity data showed the vanadyl(IV) complexes to be more potent antibacterial and antifungal than the parent Schiff bases against one or more bacterial and fungal species.     

新型缩氨基硫脲衍生物——氨基巯三唑Schiff碱的合成与抗菌活性

设计合成了新型缩氨基硫脲衍生物4-氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑及其十种不同醛的Schiff碱衍生物,并进行了抑菌实验。结果表明:Schiff碱化合物结构中的甲亚胺基是该类化合物的活性功能基。苯环上更换不同的取代基对其活性有一定的影响,其中化合物4-(5-硝基亚糠基氨基)-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ik)抗菌活性最高且抗菌谱最广;化合物4-亚水杨基氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ib)具有较强的抑霉活性。     

新型缩氨基硫脲衍生物——氨基巯三唑Schiff碱的合成与抗菌活性

设计合成了新型缩氨基硫脲衍生物4-氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑及其十种不同醛的Schiff碱衍生物,并进行了抑菌实验。结果表明:Schiff碱化合物结构中的甲亚胺基是该类化合物的活性功能基。苯环上更换不同的取代基对其活性有一定的影响,其中化合物4-(5-硝基亚糠基氨基)-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ik)抗菌活性最高且抗菌谱最广;化合物4-亚水杨基氨基-3-(呋喃-2)-5-巯基-1,2,4-三唑(Ib)具有较强的抑霉活性。     

Novel pyrazole-clubbed thiophene derivatives via Gewald synthesis as antibacterial and anti-inflammatory agents

The aim of this study was to synthesize newer potent Schiff bases by condensing 2-amino-5-(2,4-dichlorophenyl)thiophene-3-carbonitrile and 1,3-disubstituted-1H-pyrazole-4-carbaldehydes, and to investigate their biological activity. The compounds were synthesized via Gewald synthesis and characterized by spectral data and elemental analyses. They were screened for their in vitro antibacterial and anti-inflammatory activities. The synthesized compounds were also evaluated for in vitro antitubercular activity against Mycobacterium tuberculosis H37Rv using the microplate Alamar Blue assay. Compounds 8b , 8c , 8f , 8g , 8k , 8n , and 8o showed promising antibacterial activity. The interactions between the substituted pyrazoles and bovine protein showed promising anti-inflammatory activity. The experimental results revealed compound 8a as a promising antitubercular agent. Hemolytic assays confirmed that the compounds are nontoxic, with percentage hemolysis ranging from 3.6 to 20.1, at a concentration of 1 mg/ml. The results suggest that the pyrazole ring and the substitution pattern on the heterocyclic moiety have an effect on the bioactivity.     

4-Thiazolidinone and 1-thia-3,4,9-triaza fluorene conjugates: synthesis, characterization and antimicrobial screening

Some novel 4-thiazolidinone derivatives have been synthesized by the condensation of isatin/5-chloroisatin with thiosemicarbazide to yield thiosemicarbazones, which were then cyclized to form corresponding thia-3,4,9-triaza-fluoren-2-ylamines. These were reacted with substituted aldehydes to give corresponding Schiff bases, which were cyclized using thioglycolic acid in the presence of zinc chloride to obtain the 4-thiazolidinone derivatives. All the synthesized compounds were characterized by spectral (IR, MS and NMR) and elemental analysis. The compounds were screened for their antibacterial activity against Gram-positive bacteria (B. subtilis, S. aureus, B. pumilus and M. luteus), Gram-negative bacteria (P. aeruginosa, E. coli and P. fluorescens) and for antifungal activity against A. niger and P. chrysogenum by agar-diffusion method. The minimum inhibitory concentrations of these compounds were also determined by tube dilution method. The antimicrobial effectiveness of all the compounds was found to be concentration dependent. Two compounds—2-methyl-3-(1-thia-3, 4, 9-triaza-fluoren-2-yl)-thiazolidin-4-one (7aI) and 2-naphthalen-1-yl-3-(1-thia-3, 4, 9-tri aza-fluoren-2-yl)-thiazolidin-4-one (7aII)—exhibited good antibacterial activity. The antibacterial activity of all the compounds was found to be better than the antifungal activity.     

Synthesis and pharmacological evaluation of novel 1-(piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one derivatives as potential antimicrobial agents

Novel compounds of biological interest were synthesized by in situ reduction of Schiff’s base of 5,6-dimethoxy indanone and 1-(piperidin-4-yl)-1H-benzo[d]imidazol-2(3H)-one in the presence of Ti(OiPr)₄ and NaBH₃CN. Further alkylation using different alkyl/aryl halides in the presence of NaH in DMF gave a series of novel compounds. A formation of newly synthesized compounds was confirmed on the basis of their spectral and elemental analysis. Further these compounds were screened for their antimicrobial activity and found to have promising antibacterial and antifungal activity.