Investigating the spectrum of biological activity of substituted quinoline-2-carboxamides and their isosteres

In this study, a series of thirty-five substituted quinoline-2-carboxamides and thirty-three substituted naphthalene-2-carboxamides were prepared and characterized. They were tested for their activity related to the inhibition of photosynthetic electron transport (PET) in spinach (Spinacia oleracea L.) chloroplasts. Primary in vitro screening of the synthesized compounds was also performed against four mycobacterial species. N-Cycloheptylquinoline-2-carboxamide, N-cyclohexylquinoline-2-carboxamide and N-(2-phenylethyl)quinoline-2-carboxamide showed higher activity against M. tuberculosis than the standards isoniazid or pyrazinamide and 2-(pyrrolidin-1-ylcarbonyl)quinoline and 1-(2-naphthoyl)pyrrolidine expressed higher activity against M. kansasii and M. avium paratuberculosis than the standards isoniazid or pyrazinamide. The most effective antimycobacterial compounds demonstrated insignificant toxicity against the human monocytic leukemia THP-1 cell line. The PET-inhibiting activity expressed by IC(50) value of the most active compound N-benzyl-2-naphthamide was 7.5 μmol/L. For all compounds, the structure-activity relationships are discussed.     

Voltammetric determination of dinitronaphthalenes using a silver solid amalgam paste electrode

The electrochemical behavior and application of a new sensor, a silver solid amalgam paste electrode (AgSA-PE), based on the mixture of a fine silver solid amalgam powder (60:40 (w(Hg)/w(Ag))) and a suitable organic pasting liquid (Paraffin oil) in a ratio of 20:1 (w/w), was investigated in an aqueous-methanolic media (1:1). This alternative working electrode provides simple preparation and handling, adequate mechanical stability, easily renewable electrode surface, sufficiently wide cathodic potential window (up to -1200 mV within a pH range of 2.7-12.3), and sufficient sensitivity without any necessary pretreatment. The practical usability of the AgSA-PE was verified by the development of voltammetric methods for the determination of selected environmentally important pollutants (1,3-, 1,5-, and 1,8-dinitronaphthalenes) in an aqueous-methanolic media (1:1). The differential pulse voltammetric methods at AgSA-PE give linear concentration dependences in the range of 1-100 μmol l(-1) with limits of detection of about 1 μmol l(-1) in a mixture of Britton-Robinson buffer of appropriate pH and methanol (1:1).     

Non-hydrolytic synthesis of titanosilicate xerogels by acetamide elimination and their use as epoxidation catalysts

Novel non-hydrolytic syntheses of titanosilicate xerogels by polycondensation of silicon acetate, Si(OAc)₄, with titanium (IV) dimethylamide or diethylamide, Ti(NR₂)₄ (R?=?Me, Et), are presented. The reactions are based on acetamide elimination and yield gels with a high content of Si?CO?Ti bonds in comparison with the ester elimination route. Although a ligand exchange was observed, it was interestingly not followed by homo-condensation and during the synthesis the phase separation to SiO₂ and TiO₂ was avoided. The degree of condensation reached up to 68?%. The xerogels prepared for a comparison by ester elimination from Si(OAc)₄ and titanium (IV) isopropoxide featured a significantly lower content of the Si?CO?CTi bonds. The initial tests in the epoxidation of cyclohexene by cumyl hydroperoxide (CHP) indicated a high selectivity and moderate activity of the xerogels. The catalytic properties were significantly improved by combining non-hydrolytic and hydrolytic methods yielding mesoporous and homogeneous Si/Ti mixed oxides. The catalysts prepared by these methods provided a complete epoxidation of cyclohexene in 2?h at?65?°C.     

Linear parameter varying control design for rotating systems supported by journal bearings

Linear parameter varying (LPV) control is a model-based control technique that takes into account time-varying parameters of the plant. In the case of rotating systems supported by lubricated bearings, the dynamic characteristics of the bearings change in time as a function of the rotating speed. Hence, LPV control can tackle the problem of run-up and run-down operational conditions when dynamic characteristics of the rotating system change significantly in time due to the bearings and high vibration levels occur. In this work, the LPV control design for a flexible shaft supported by plain journal bearings is presented. The model used in the LPV control design is updated from unbalance response experimental results and dynamic coefficients for the entire range of rotating speeds are obtained by numerical optimization. Experimental implementation of the designed LPV control resulted in strong reduction of vibration amplitudes when crossing the critical speed, without affecting system behavior in sub- or super-critical speeds.     

Health Beneficial Properties of Grapevine Seed Extract and Its Influence on Selected Biochemical Markers in the Blood,Liver and Kidneys of Rattus norvegicus

Cadmium (Cd) is a heavy metal that occurs in all areas of the environment, including the food chain. In the body, it causes oxidative stress by producing free radicals that are harmful to the cells. Grape seed extract (GSE) contains a wide range of biologically active components that help to neutralize the adverse effects of free radicals. In this study, the effects of GSE prepared form semi-resistant grapevine cultivar Cerason, which is rich in phenolics, on biochemical markers of brown rats exposed to the effects of cadmium were monitored. GSE increased the plasma antioxidant activity and, in the kidneys and the liver, Cd content was significantly lowered by GSE co-administration. Accordingly, the increase in creatinine content and alanine aminotransferase activity and the decrease of catalase and superoxide dismutase activities caused by cadmium were slowed down by GSE co-administration. The results of this work reveal that grape seed extract offers a protective effect against the intake of heavy metals into the organism.     

Path integrals for the continuous spontaneous localization theory

Path integral expressions are given for the wave function and for the density matrix in a theory which describes state vector reduction. The magnitude of the contribution of each classical path to the propagator is not unity, as in ordinary quantum theory, but depends upon the path.     

Atomic-Scale Studies of Fe3O4(001) and TiO2(110) Surfaces Following Immersion in CO2-Acidified Water

Difficulties associated with the integration of liquids into a UHV environment make surface-science style studies of mineral dissolution particularly challenging. Recently, we developed a novel experimental setup for the UHV-compatible dosing of ultrapure liquid water and studied its interaction with TiO₂ and Fe₃O₄ surfaces. Herein, we describe a simple approach to vary the pH through the partial pressure of CO₂ ( ) in the surrounding vacuum chamber and use this to study how these surfaces react to an acidic solution. The TiO₂(110) surface is unaffected by the acidic solution, except for a small amount of carbonaceous contamination. The Fe₃O₄(001)-( × )R45° surface begins to dissolve at a pH 4.0–3.9 ( =0.8–1 bar) and, although it is significantly roughened, the atomic-scale structure of the Fe₃O₄(001) surface layer remains visible in scanning tunneling microscopy (STM) images. X-ray photoelectron spectroscopy (XPS) reveals that the surface is chemically reduced and contains a significant accumulation of bicarbonate (HCO₃⁻) species. These observations are consistent with Fe(II) being extracted by bicarbonate ions, leading to dissolved iron bicarbonate complexes (Fe(HCO₃)₂), which precipitate onto the surface when the water evaporates.     

Use of iterative natural orbital method for calculating energy barrier to predissociation of the first excited states of NH3 (3s1,3 A″2)

The barrier to predissociation of the first excited states of NH₃ (3s^1,3 A) is computed from a truncated first-order wave function using the iterative natural orbital method. The results show that the barrier is lower than when calculated with RHF and the CI wave functions, where single and double replacements to a truncated virtual space are carried out. These findings are used to interpret experimental data.     

Voltammetric Determination of 3‐Nitrofluoranthene and 3‐Aminofluoranthene at Boron Doped Diamond Thin‐Film Electrode

The voltammetric behavior of 3‐nitrofluoranthene and 3‐aminofluoranthene was investigated in mixed methanol‐water solutions by differential pulse voltammetry (DPV) at boron doped diamond thin‐film electrode (BDDE). Optimum conditions have been found for determination of 3‐nitrofluoranthene in the concentration range of 2×10^?8–1×10^?6 mol L^?1, and for determination 3‐aminofluorathnene in the concentration range of 2×10^?7–1×10^?5 mol L^?1, respectively. Limits of determination were 3×10^?8 mol L^?1 (3‐nitrofluoranthene) and 2×10^?7 mol L^?1 (3‐aminofluoranthene).