Journal of Thermal Analysis and Calorimetry - In recent decades, the growth of heat transfer using nanomaterials in the conventional base fluid has caught the attention of researchers... 相似文献
A new series of quinolotacrine hybrids including cyclopenta- and cyclohexa-quinolotacrine derivatives were designed, synthesized, and assessed as anti-cholinesterase (ChE) agents. The designed derivatives indicated higher inhibitory effect on the acetylcholinesterase (AChE) with IC50 values of 0.285–100 µM compared to butyrylcholinesterase (BChE) with IC50 values of?>?100 µM. Of these compounds, cyclohexa-quinolotacrine hybrids displayed a little better anti-AChE activity than cyclopenta-quinolotacrine hybrids. Compound 8-amino-7-(3-hydroxyphenyl)-5,7,9,10,11,12-hexahydro-6H-pyrano[2,3-b:5,6-c'] diquinolin-6-one (6m) including 3-hydroxyphenyl and cyclohexane ring moieties exhibited the best AChE inhibitory activity with IC50 value of 0.285 µM. The kinetic and molecular docking studies indicated that compound 6m occupied both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of AChE as a mixed inhibitor. Using neuroprotective assay against H2O2-induced cell death in PC12 cells, the compound 6h illustrated significant protection among the assessed compounds. In silico ADME studies estimated good drug-likeness for the designed compounds. As a result, these quinolotacrine hybrids can be very encouraging AChE inhibitors to treat Alzheimer’s disease.
Graphic abstract
A novel series of quinolotacrine hybrids were designed, synthesized, and evaluated against AChE and BChE enzymes as potential agents for the treatment of AD. The hybrids showed good to significant inhibitory activity against AChE (0.285–100 μM) compared to butyrylcholinesterase (BChE) with IC50 values of?>?100 μM. Among them, compound 8-amino-7-(3-hydroxyphenyl)-5,7,9,10,11,12-hexahydro-6H-pyrano[2,3-b:5,6-c′] diquinolin-6-one (6 m) bearing 3-hydroxyphenyl moiety and cyclohexane ring exhibited the highest anti-AChE activity with IC50 value of 0.285 μM. The kinetic and molecular docking studies illustrated that compound 6 m is a mixed inhibitor and binds to both the catalytic anionic site (CAS) and peripheral anionic site (PAS) of AChE.
The joint probability distribution function (PDF) of the height and its gradients is derived for a zero tension d + 1-dimensional Kardar-Parisi-Zhang (KPZ) equation. It is proved that the height's PDF of zero tension KPZ equation shows lack of positivity after a finite time tc. The properties of zero tension KPZ equation and its differences with the case that it possess an infinitesimal surface tension is discussed. Also potential relation between the time scale tc and the singularity time scale tc.v→0 of the KPZ equation with an infinitesimal surface tension is investigated. 相似文献
This work is part of a project with the IAEA, in a coordinated program on Trace Elements in Human and Bio-Environmental Systems to evaluate their nutritional requirements, interrelations and the role of trace elements in health, metabolism, etc. Cow's milk being regarded as one of the most important and nutritious foodstuffs consumed by people. Hence as a first step, an elemental analysis for milk was carried out for this purpose; a few samples of pasteurized milk and local sample were investigated for essential and toxic trace elements. The secondary aim of this project was the assessment of various analytical techniques involved. However, in the present work, the methods involved were AAS, PIXE and NAA. The latter method was applied both instrumentally and radiochemically. Although the results pertaining to the various methods employed are not in good agreement. there is, however, some justification to clarify this internal inconsistency. The precision of NAA and AAS allows a greater degree of acceptance. Although PIXE is very fast and rather routine, the technique for trace element analysis needs certain adaptations and development. 相似文献
The potentiometric response properties and applications of a tetra-coordinate nickel(II) complex with relatively high selectivity toward nitrate ion are described. The nickel(II) complex of 5,7,12,14-tetramethyl-1,4,8,11-tetraazacyclotetradeca-4,6,11,13-tetraene was used as a neutral carrier into plasticized poly(vinyl chloride) (PVC) membrane. The influence of several variables was investigated in order to optimize the potentiometric response and selectivity of the electrode. The resulting membrane electrode incorporating 31.0% PVC, 61.0% dioctyl phthalate (DOP) as plasticizer, 3% methyltrioctylammonium chloride (MTOAC) as a cationic additive and 5% carrier (all w/w) demonstrates a Nernstian response slope of −59.6 mV per decade over the concentration range of 5×10−6-1×10−1 M NO3−. The electrode exhibits a fast response time (≤10 s), a detection limit of 2.5×10−6 M, and can be used over a wide pH range of 4-12. The electrode shows improved selectivity in comparison to most of the previously reported nitrate-selective electrodes. It was successfully applied to the determination of nitrate ion in natural water samples. 相似文献
The singlet oxygen (1Δg) photooxidations of angelic acid salt (1), tiglic acid salt (2), 2,3-dimethyl-2-butenoic acid salt (3), 3-ethoxycarbonyl-5,6-dihydro-2-methyl-4H-pyrane acid salt (4), cis-3-hexenoic acid salt (5), and trans-3-hexenoic acid salt (6) were conducted in deuterated water. The major and minor ene allylic hydroperoxide products were quantified and indicate that the allylic hydrogen geminal to the carboxylate group is preferentially abstracted in 1-4, whereas the allylic hydrogen α to the carboxylate is slightly favored for 5 and 6. We have attributed the observed regiochemistry in 1-4 to stabilizing hydrogen bonding interactions between the solvent and the perepoxide, which leads to the major ene product. 相似文献
A narrow bandwidth ring dye laser pumped by an argon ion laser has been used to investigate the hyperfine structure of the even and odd parity levels of tantalum by optogalvanic spectroscopy in the wavelength range 5640 to 6050 Å. Seventeen transitions have been observed and eight of these have not been reported in the literature so far. These transitions involve 27 levels with 15 odd and 12 even parity configurations. The magnetic dipole hyperfine interaction constants A and the electric quadrupole interaction constants B for these levels have been computed and compared with the data available in literature. The results for the levels at 34799.71 cm?1, 26960.46 cm?1 and 19657.78 cm?1 are reported for the first time. 相似文献
Flameless atomic absorption techniques were used to determine the lead and other atmospheric particulate in the city of Tehran. 640 samples were collected in 20 different stations around the city during four seasons in 1992. The radioactivity of the air samples was also measured by -ray spectrometry using high purity Ge/Li detectors, and a multichannel analyzer. The results were compared with previous measurements in the city of Tehran. 相似文献
Radiotracer method was developed for measuring14CO2 content in cement-wood mixtures. The carbon dioxide used for the treatment was labeled with14C, a -emitting radioisotope, and samples were measured by -scintillation and liquid scintillation techniques. Test samples were prepared in the laboratory with various compositions and treated with labeled14CO2. The tracer was released from Ba14CO3 by lactic acid with total activity of 37 MBq. Selectivity of the technique allows to distinguish the carbon dioxide bound during the treatment and bound previously from the mbient air. Sensitivity of the method is higher than that of traditional methods and allowed determination of CO2 content in each component of the mixture. It is 63 ng. if measured by -scintillation detector and 1.6 ng, if measured by liquid scintillation. Accuracy of the method is 0.3%. 相似文献
A new method for the rapid and sensitive determination of trace quantities of thiocyanate based on its Landolt effect on the bromate-hydrochloric acid reaction was developed. The induction period of the reaction is proportional to the SCN– concentration. The decolorization of methyl orange by the reaction products was used to monitor the reaction spectrophotometrically at 525 nm. We were able to determine thiocyanate in the range 2 × 10–7–4 × 10–5 M by this method. The relative standard deviation for 10 determinations of 1.5 × 10–6 M thiocyanate ion is 0.19% and the detection limit of the method was 7.00 × 10–8 M. The method was applied to the determination of thiocyanate in human blood serum and of saliva samples with satisfactory results. 相似文献