Synthesis and biological screening of 7-hydroxy-4-methyl-2H-chromen-2-one, 7-hydroxy-4,5-dimethyl-2H-chromen-2-one and their some derivatives

7-Hydroxy-4-methyl-2H-chromen-2-one (2), 7-hydroxy-4,5-dimethyl-2H-chromen-2-one (15) and their some derivatives were synthesized for exploring selected biological screening. The compounds 9 and 13 had shown high degree of cytotoxic activity. Three compound 9, 10 and 13 showed high degree of bactericidal activity amongst the present series.     

Electrocatalytic oxidation of ascorbate by heme-FeIII/heme-FeII redox couple of the HRP and its effect on the electrochemical behaviour of an L-lactate biosensor

The measurements of L-lactate using the carbon paste electrode modified with lactate oxidase (LOD), horseradish peroxidase (HRP) and ferrocene (FcH) operating at low working potential in flow injection mode showed that the intensity as well as the shape of peaks were dependent on the concentration of the reducing species present in samples (e.g. ascorbate) even at low operating potentials (-200 to 0 mV vs. Ag/AgCl). The mechanism of the electrochemical contribution of ascorbate to the L-lactate response was examined by using cyclic voltammetry, hydrodynamic voltammetry and FIA results. Comparative studies showed that HRP was catalytically active for the oxidation of ascorbate leading to a decrease in the cathodic electrochemical signal of L-lactate. The results of our investigation postulated that the direct electron transfer from the HRP-Fe(III)/HRP-Fe(II) redox couple to the electrode surface was involved in the electrocatalytic oxidation of ascorbate at the electrode surface.     

Surfactant effects of chlorpromazine and imipramine on lipid bilayers containing sphingomyelin and cholesterol

The surface-active drugs chlorpromazine (CPZ) and imipramine (IP) have been tested on large unilamellar vesicles composed of phosphatidylcholine (PC), sphingomyelin (SM), and cholesterol (Ch) in different proportions. The well-characterized nonionic detergent Triton X-100 (TX) has also been used in parallel experiments. Leakage of vesicular aqueous contents and bilayer solubilization have been measured for each surfactant molecule and vesicle composition. All three surface-active molecules behave in a qualitatively similar way, irrespective of bilayer composition: they induce leakage at concentrations well below their critical micellar concentrations (cmc) and solubilization near the cmc. In these events, the potency of the three surfactants under study increases with decreasing cmc, in the order IP相似文献   

Kinetic Spectrophotometric Determination of Ranitidine

Two spectrophotometric methods were developed for the determination of ranitidine. The first method was a kinetic spectrophotometric method based on the catalytic effect of ranitidine on the reaction between sodium azide and iodine in an aqueous solution. The calibration graph was linear from 4–24 μg/mL. The drug was determined by measuring the decrease in the absorbance of iodine at 348 nm using a fixed time method. The decrease in the absorbance after 1 minute from the initiation of the reaction was related to the concentration of drug. The detection limit of the procedure was 0.76 μg/mL. The proposed procedure was successfully utilized in the determination of the drug in pharmaceutical preparations with mean recovery in the range of 99.83 ? 101.16%. The second method is a colorimetric method, which depends on the measurement of absorbances of tris (o‐phenanthroline) iron(II) [method 2A] and tris (bipyridyl) iron(II) [method 2B] complexes at 512 nm. The complexes obeyed Beer's law over the concentration range of 2–16 μg/mL and 4–40 μg/mL for methods 2A and 2B, respectively. The developed method has been successfully applied for the determination of ranitidine in bulk drugs and pharmaceutical formulations. The common excipients and additives did not interfere in its determination.     

Mass spectra of trimethylsilyl derivatives of naturally occurring flavonoid aglycones and chalcones

Electron impact mass spectra of the trimethylsilyl derivatives of a series of flavonoid aglycones and chalcones are reported. The spectra show prominent ions arising from fragmentation of the trimethylsilyl (TMS) groups. Inter-actions between adjacent TMS groups, and between TMS groups in the 3- or 5-position (6′-position for the chalcones) and the C-ring carbonyl, yield structurally significant ions. Few fragments associated with the retro-Diels-Alder cleavage of the C-ring characteristic of the underivatized compounds, are observed. The TMS derivatives thus provide complementary information for the identification of flavonoid aglycones and chalcones in biological systems.     

Selective hydroformylation–acetalization of aryl alkenes in methanol catalyzed by RhCl3·3H2O–P(OPh)3 system

Acetals were formed under hydroformylation conditions of alkenes in alcohols as solvents. The hydroformylation process is combined with acetalization in a one-pot reaction leading to acetals as final products. These reactions sequences were catalyzed by the simple rhodium catalyst RhCl₃·3H₂O. The effects of the addition of different types and amounts of phosphine and phosphite ligands were carefully studied in order to improve the regioselectivity of the reaction.     

Studies with Polyfunctionally Substituted Heterocycles: New Synthesis of Pyrido[5′, 4′:2,3][1,3,4]oxadiazolo[3,2-a]pyridine; Pyridazine; 1,3,4-Oxadiazote; and Pyrazolo[1,5-a]Pyrimidine Derivatives

Cyanoacetohydrazide 1a reacts with 2-arylhydrazoketons 2a,b and 3a,b in refluxing ethanol to yield pyrido[5′,4′:2,3][1,3,4]oxadiazolo[3,2-a]pyridine and pyridazine derivatives; in the absence of solvent pyrazolo[1,5-a]pyrimidine derivatives were obtained. The reaction of 2a,b and 3a,b will) benzoylhydrazine afforded 1,3,4-oxadiazole and pyrazole derivatives.     

Determination of traces of Zn, Cd, Pb and Cu in white sugar by anodic stripping voltammetry and a modified oxygen-flask combustion technique

Anodic stripping voltammetry with a hanging-drop mercury electrode is used for determination of traces of Zn, Cd, Pb and Cu in white sugar. The sample (1.5 g) is decomposed by ignition in oxygen in a specially modified system.     

Separation and Chemical Characterization of Wetting Crude Oil Compounds

To improve the understanding of wettability, especially the influence of colloidal stability and composition of crude oil, wetting experiments on quartz sand were performed with an asphaltene-rich oil, a resin-rich oil, and with model oils containing different colloid compositions. A two-step procedure was developed to investigate the wetting behavior. In the first step those crude oil components were extracted, which preferentially wet solid surfaces. The extracted crude oil components were characterized in the second step. The amount of adsorbed oil components correlates with the stability of the crude oil colloids: low colloidal stability of crude oil leads to larger amounts of adsorbed components than does high colloidal stability. The addition of resins and/or low molecular weight asphaltenes to the crude oil stabilizes the crude oil colloids; i.e., a lower amount of wetting components are isolated by extraction in such systems. To find out, which fraction of the adsorbed oil components determines the wetting behavior of a crude oil, the wetting properties of the toluene solutions of these fractions were compared to those of the toluene solutions of the precipitated crude oil colloids. The fractions extracted with the solvent systems chloroform and methanol/chloroform showed nearly the same wetting behavior as the crude oil colloids. These fractions are characterized by the highest molecular weights, higher sulfur compositions, and the lowest H/C ratios. On the other hand, the nitrogen compounds predominate in the acetone fraction.     

Direct conjugation of semiconductor nanoparticles with proteins

Nanocrystalline CdS particles directly conjugated with bovine serum albumin (BSA) protein were prepared by applying the supercritical fluid processing technique, rapid expansion of a supercritical solution into a liquid solvent. The direct conjugation takes advantage of the unique features of the process for nanoparticle formation. The BSA-conjugated CdS nanoparticles in stable aqueous suspension or in the solid state were characterized by using microscopy, X-ray diffraction, and optical spectroscopy methods. The results show that well-dispersed CdS nanoparticles are coated with BSA in a core-shell-like arrangement and that the protein species associated with the nanoparticles remain functional according to the modified Lowry assay. These BSA-conjugated CdS nanoparticles are also strongly luminescent, with the luminescence spectrum contributed to primarily by the exciton emission.