3-Cyano-4,6-disubstituted 4H-pyrans are endowed with a variety of pharmacodynamic activities Looking to the interesting properties of cyanopyrans, it was considered worthwhile to synthesis some new 2"-amino-4"-[2-(4'-chlorophenyl) -6-methyl imidazo [1,2-a] pyridin-3-yl]-6"-aryl-4"-H-pyran-3"- carbonitrile ( 4a-4l ) have been synthesized. The products have been assayed for their biological activity against Gram +ve, Gram –ve bacteria and fungi. Some of the products showed moderate activity in concentration 50μg/mL. The structures of the products have been elucidated by IR, 1H-NMR, Mass spectral data, elemental analysis and thin layer chromatography.
Condensation of 5-nitro-, 3-chloro-, and 5-chlorosalicylic acids with formaldehyde afforded dimeric disalicylmethanes, which were O-methylated with dimethyl sulfate and oxidized with chromium(VI) oxide to diarylketones 9,10,11,12. Wittig reaction with ylides obtained by deprotonation of alkyltriphenylphosphoniu salts with sodium bis(triethylsilyl)amide yielded a series of diarylalkenes. Some of the obtained compounds showed high antibacterial activity in vitro against Erwinia carotovora.
InWO3-InMoO3 loaded-TiO2 nanomaterial was synthesised by co-precipitation method and sonication technique. The nanomaterial was characterized by High-resolution scanning electron microscopy (HR-SEM) with elementary dispersive X-ray (EDX), High-resolution transmission electron microscopy (HR-TEM), photoluminescence spectroscopy (PL) and UV-Vis diffuse reflectance spectroscopy (DRS). The photocatalytic activity of InWO3-InMoO3 loaded-TiO2 nanomaterial was studied from the photodegradation of methyl green (MEG) and methylene blue (MB) under UV-light irradiation at 365 nm. The hydroxyl radical formation in the mechanism was confirmed by fluorescence quenching technique. The mineralization confirmed by chemical oxygen demand measurements. A flaxisible mechanism is proposed for higher catalytic activity of InWO3-InMoO3-TiO2 under UV-light for 365 nm. This catalyst was found to be stable and reusable without appreciable loss of catalytic activity up to five cycles. The InWO3- InMoO3 loaded-TiO2 nanomaterial on MEG was high photocatalytic activity that of MB so high photocatalytic activity has been discussed by first order kinetics, rate constant value and high quantum yield. This material was showed increased hydrophobicity that of TiO2 electrochemical study and antibacterial activity of the analysis was also studied.
The triorganotin(IV) com plex of com po si tion Ph3Sn(OArMe-4) has been synthesized in good yields by the reaction of Ph3SnCl with Me3SiOArMe-4/NaOArMe-4, while complexes of composition Me3Sn(OArMe-4) and n-Bu3Sn(OArMe-4) (where -OArMe-4 = -OC6H4CH3-4) have been obtained from the reaction of Me3SnCl and n-Bu3SnCl with 4-methylphenol in the presence of triethylamine in carbon tetrachloride. The complexes have been characterized by elemental analyses, molar conductance measurements, molecular weight determin tion and IR, 1H and 13C NMR and mass spectral studies. Thermal behaviour of the complexes has been studied by TG and DTA techniques. The organotin(IV) complexes have also been screened for their antibacterial properties and are found to exhibit appreciable activity. The reactions of the complexes with 2-, 3-, 4-cyanopyridines yielded 1:1 adducts as confirmed by physicochemical and IR spectral data.
A new series of four transition metal complexes of a Schiff base derived from salicylaldehyde and glycine, viz. [N-salicylidene glycinato diaqua cobalt (II) dimer] (SGCo)2, [N- salicylideneglycinato-di-aqua-nickel(ll)dimer] (SGN)2, [N-salicylideneglycinato-aqua-copper(II)] (SGC) and [N-salicylidene glycinato diaqua zinc(II) dimer] (SGZ)2 have been synthesized and characterized through a rapid, simple, and efficient methodology in excellent yield. These compounds were screened for in vitro antibacterial activities against six pathogenic bacteria, such as Shigella sonnei, Escherichia coli, Bacilus subtilis, Sarcina lutea, Staphylococcus aureus and Pseudomonas arioginosa. The antibacterial activity was determined by the disc diffusion method using DMSO as solvent. The results indicate that (SGC) compound exhibit a significant antibacterial activity, depending on the bacterial strain and (SGCo)2, (SGN)2 and (SGZ)2 compounds show a moderate sensitivity even with higher doses. All these compounds were found to possess cytotoxic effect.
Poly ethylene oxide is an uncrosslinked, non-ionic linear hydrophilic polymer with a variety of molecular weights. PEO is used to make it, and it offers a number of beneficial qualities for medication delivery and antibacterial uses. The antibacterial activity of polyethylene oxide (PEO) at various concentrations as (80, 40, 20, 10 g/ml) against bacteria in Gram-positive Staphylococcus aureus, Streptococcus pyogenes and Lactobacillus sp. and Gram-negative Enterobacter bugandensis, E. coli, Pseudomonas aeruginosa and Klebsiella pneumonia was investigated in this study. The disk diffusion experiment was used to assess the antimicrobial activity of PEO, as well as each isolate’s minimum inhibitory concentration (MIC) and minimum bactericidal concentration (MBC). PEO is shown to have strong broad-spectrum antibacterial action against the bacteria studied, that inhibition zone increase their width inversely proportional to PEO concentration, and has even outpaced the efficacy of certain medicines. PEO had MICs ranging from 10 to 20 g/ml, as well as MBCs of 20 to 80 g/ml. In additional studies, PEO was discovered to be strongly associated with the cell of bacteria, which contributed to its inhibitory impact on bacterial invasion and growth. PEO at an appropriate dose effectively decreased bacterial growth. PEO is highly recommended as a cost-effective antibacterial treatment, Specifically, ectopic infection treatment without the risk of bacterial strains becoming antibiotic-resistant.
Two Schiff base com pounds, C15H12BrClN2O3×2CH3OH (1) and C14H10BrClN2O3×CH3OH (2), have been synthesized by the condensation reactions of equimolar quantities of 3-bromo-5-chlorosalicylaldehyde with 3-methoxy benzohydrazide and 3-hydroxy - benzohydrazide, respectively, in methanol solutions. Compound (1) consists of a Schiff base molecule and two metha ol molecules of crystallization, while compound (2) con - sists of a Schiff base molecule and one methanol molecule of crystallization. Both com - pounds were characterized by elemental analysis, IR spectra and single-crystal X-ray diffractions. As expected, each Schiff base molecule adopts an E-configuration about the C=N double bond. In both crystal structures, molecules are linked through intermolecular hydrogen bonds and weak Br×××O or Br×××Br interactions, forming layers. Both compounds possess potent antibacterial activities.
A series of novel complexes of 4-amino-5-benzyl-4H-1,2,4-triazole-3-thione (ABT), 5-benzyl-4-(benzylideneamino)-4H-1,2,4-triazole-3-thione (BBT), 5-benzyl-4-[(2- hydroxybenzylidene)amino]-4H-1,2,4-triazole-3-thione (HBHT) and 5-benzyl-4-[(4- methoxybenzylidene)amino]-4H-1,2,4-triazole-3-thione (BMT) with the divalent ions Co(II), Ni(II), Cu(II) and Cd(II) have been prepared by direct combination of the ligand and metal chloride salt in ethanol. The structures were determined by elemental analysis, molar conductance, magnetic measurements, thermal behaviour, infrared and electronic spectral data. ABT involves N (amino group) and S donor atoms, BBT and BMT involve N (azomethine) and S donor atoms, both act as neutral bidentate ligands. HBHT involves N, O and S donor atoms, acting as monobasic tridentate ligands. The stoichiometry of these complexes is M:L= 1:1 and/or 1:2. The geometry of the complexeswas assigned on the basis of magnetic and electronic spectral data. Tetrahedral and octahedral structures were proposed for the metal complexes. The ligands and their complexes were screened for their antibacterial activity.
New multidentate ligands 1,4,7,9,12-pentaaza-10,11-dioxo-8,9,12,13-bis-(1_,3_-dioxo- 6,6-diethyl-2_-hydropyrimidine)-trideca-7,13-diene, (L1) and 1,4,7,9,13-pentaaza-10,12- dioxo-8,9,13,14-bis-(1_,3_-dioxo-6,6-diethyl-2_-hydropyrimidine)-tetradeca-7,14-diene (L2) have been prepared by the reaction of 5,5-diethylbarbituric acid, diethylenetriamine, diethyl oxalate and 5,5-diethylbarbituric acid, diethylenetriamine, diethyl malonate. Their coordination properties with the first row of transition metal ions have been explored. The macrocyclic complexes were characterized by elemental analysis, IR, 1H NMR, UV-visible spectroscopy, magnetic moment measurements and molar conductance measurements. The electronic spectra and magnetic moment measurements are discussed with respect to assignment of square planar and tetrahedral structure except chromium(III), iron(III) ions. The chromium(III) and iron(III) complexes are considered to be octahedral. Molar conductance measurements suggest that the complexes of divalent metal ions are 1:1 electrolytes, while the trivalent metal ions are nonelectrolytes. The compounds have been tested against gram-positive bacteria Staphylococcus aureus and gram-negative bacteria Escherichia coli. The results show that all the compounds inhibit the growth of bacteria.
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Silver nanoparticles (NPs) have at least one dimension of a particle smaller than 100 nm and contain 20-15,000 silver atoms. Due to its antibacterial activity nanosilver (NS) is used for medical purposes. NS particles can be obtained by various methods. Potentially, the best method of the NS synthesis for medical purposes is based on a brief flow of electric current between two silver electrodes placed in deionized water. It is accepted that the major antibacterial effect of silver is its partial oxidation and releasing silver ions, which interact with thiol groups of peptidoglicans of bacterial cell wall, and proteins of the cell membrane causing cell lysis. Silver ions can also bind to bacterial DNA preventing its replication and stopping synthesis of bacterial proteins. The rise in exposure to silver NPs has spurred interest into their toxicology. NS undergoes a set of biochemical transformations including accelerated oxidative dissolution in gastric acid, binding to thiol groups of serum and tissue proteins, exchange between thiol groups, sulfides and selenides, binding to selenoproroteins and photoreduction in skin to zerovalent metallic silver. Animal studies have shown that exposure to NS may lead to liver and spleen damage. NS can also stimulate an increased secretion of proinflammatory cytokines by monocytes. As a spectrum of NS applications is still growing, the complex evaluation of a safety of its use becomes an important task. This requires an elucidation of not only the influence of NS on human cells and organism, but also its biotransformation in organism and in environment.
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Isoxazoline derivatives shows various types of therapeutic activities like antimicrobial[1], antiinflammatory[ 2], anticonvulsant[3], Hypoglycemic[4] etc. getting to synthesized in view of 3-Aryl-5[(4′-difluoromethoxy)(3′-hydroxy)phenyl]-4,5-dihydro isoxazole (4a-4i) have been synthesized. All the newly synthesized compounds were screened for their antibacterial activity against S. aureus, M. luteus (Gram-positive bacteria), E. coli, S. thyphi (Gram-negative bacteria) and antifungal activity against Candida albicans (Fungi). The biological activities (MIC) of the synthesized compounds were compared with known standard drugs.
Celem pracy była ocena aktywności przeciwbakteryjnej modyfikowanego lizozymu w stosunku do bakterii Gram-ujemnych Pseudomonas fluorescens i Proteus mirabilis. Porównano antybakteryjne działanie monomeru lizozymu i jego preparatu uzyskanego w wyniku modyfikacji termiczno-chemicznej. W otrzymanym preparacie lizozymu oznaczono udział form oligomerycznych, aktywność hydrolityczną i hydrofobowość. Stwierdzono wzrost inhibitującego działania lizozymu po modyfikacji w porównaniu z monomerem lizozymu i próbą bez dodatku enzymu w stosunku do badanych bakterii. Wykazano, że modyfikowany preparat lizozymu wykazujący aktywność przeciwbakteryjną wobec bakterii gramujemnych, charakteryzuje się wyższym udziałem form oligomerycznych jak również wyższą hydrofobowością powierzchniową.
EN
The aim of the study was to assess the antibacterial activity of modified lysozyme in relation to Gram-negative bacteria Pseudomonas fluorescens and Proteus mirabilis. Antibacterial action of lysozyme monomer and its preparation produced as a result of thermo-chemical modification were compared. In the obtained lysozyme preparation the proportion of oligomeric forms, hydrolytic activity and hydrophobicity were determined. An increase was found in the inhibitory action of lysozyme after modification in comparison with lysozyme monomer and the sample without an addition of the enzyme in relation to the analysed bacteria. It was shown that the modified lysozyme preparation exhibiting antibacterial activity against Gram-negative bacteria is characterised by a higher proportion of oligomeric forms, as well as higher surface hydrophobicity.
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Two series of benzimidazole derivatives were sythesised. The first one was based on 5,6-dinitrobenzimidazole, the second one comprises 2-thioalkyl- and thioaryl-substituted modified benzimidazoles. Antibacterial and antiprotozoal activity of the newly obtained compounds was studied. Some thioalkyl derivatives showed remarkable activity against nosocomial strains of Stenotrophomonas malthophilia, and an activity comparable to that of metronidazole against Gram-positive and Gram-negative bacteria. Of the tested compounds, 5,6-dichloro-2-(4-nitrobenzylthio)-benzimidazole showed the most distinct antiprotozoal activity.
The sol-gel derived silica spheres with surfaces modified by silver nanoparticles were used to enhance the photodynamic effect. The silica nanoparticles were prepared by modified Stöber synthesis. The diameter of obtained silica spheres was ca. 100 nm. These silica spheres we used as a carrier for noble nanoparticles. It was shown that Ag-Au nanoparticles have an antibacterial activity against Escherichia coli. This effect depends on the nanoparticles concentration and it is stronger for higher concentrations. Laser irradiation enhances this effect, and starting from certain concentration it is possible to kill Escherichia coli, totally, when using laser light.
Three Schiff bases derived from thiosemicarbazide and ketones (Vanillin, Benzophenone and Acetophenone) were used to study their antibacterial activities against some pathogenic bacteria by disc diffusion method. Of these, benzophenone thiosemicarbazone showed significant antibacterial activity as compared with that of Kanamycin. All these three compounds were found to possess cytotoxic effect. Minimum inhibitory concentration of these compounds was also determined.
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N-Substituted phenyl/cyclohexyl-2-(pyridine-4-carbonyl) hydrazine-1-carbothioamides (2a–r) were synthesized, characterized by spectral and analytical data. The compounds were evaluated for antibacterial activity by the discdiffusion method. Most of the compounds showed activity against Gram-positive bacteria. Compound 2h with 4-Sulfapyrimidine phenyl substitution was found to be the most promising candidate, active against Gram-positive and methicillin-resistant Staphylococcus aureus (MRSA) strains with minimum inhibitory concentration (MIC) of (2–7 μg/mL). From the docking study, we predicted that compounds (2r, 2g, 2h, 2o, 2p and 2e) possess better antibacterial activity by having a good binding affinity with target protein and they could be used as potential drugs as antimicrobials. Amongst all the docked compounds, the compound 2h presented near binding affinity & interaction docking score with DNA gyrase enzymes with reference to ciprofoxacin.
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Pyridine nucleus plays an important role in medicine, agriculture and industrial chemistry. With a view of biological activities and variety of industrial applications, some new 2" – methoxy - 4" - [2 - ( 4' -chlorophenyl)-6-methyl imidazo [1, 2-a] pyridin-3-yl]-6"-aryl nicotinonitrile( 4a-4l ) has been synthesized. The products have been assayed for their biological activity against Gram +ve, Gram –ve bacteria and fungi. Some of the products showed moderate activity in concentration 50µg/ml. The structures of the products have been elucidated by IR, 1H-NMR, Mass spectral data, elemental analysis and thin layer chromatography.
Two novel dinuclear Schiff base complexes, [Ni2L2(NCS)2] (1) and [Cu2L2(NCS)2] (2), where L = 2-[(2-dimethylaminoethylimino)methyl]phenolate, have been synthesized and characterized by elemental analyses, IR, and single crystal X-ray diffraction. They are structurally similar. Each of the two metal ions of the complex is coordinated by two nitrogen and two oxygen atoms in the basal plane of a distorted square pyramid and by one nitrogen atom in its apex. The oxygen atoms belong to two Schiff base ligands and form bridges between two metal ions, while the nitrogen atoms of the basal plane belong to one ligand coordinated to a given metal atom. The apex nitrogen is that of the thiocyanate anion. The Schiff base and the two complexes showed effective antibacterial activities. It is noteworthy that the two complexes have stronger antibacterial activities than that of the corresponding Schiff base ligand.
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Extracts obtained from hops (Humulus lupulus L., Cannabaceae) by supercritical fluid extraction (SFE), SFE followed by isomerization, as well as by conventional technique, were investigated for their chemical composition and antibacterial activity against selected foodborne pathogens and microorganisms capable to cause the food spoilage. The antibacterial activity of the extracts was compared with the antibacterial activity of xanthohumol, compound known for its broad pharmacological properties, isolated from the raw material remained after the SFE. Xanthohumol (XH, 96%) proved to posses the most prominent activity against all the tested strains, with the MIC values ranged between 2.5 and 20 μg mL-1. Supercritical hops extract and potassium isomerized supercritical hops extract showed strong antibacterial activity against the tested strains as well. Escherichia coli was not affected by the extracts, meaning that their oral admission would not cause the same problem as antibiotic application in intestinal flora. The chemical composition of the investigated hops extracts was analysed by GC-MS. Contents of α-acids, β-acids, iso-α-acids and xanthohumol in the samples were determined by HPLC.
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