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 performance of octahydroxycalix[4]arene derivative used as a neutral carrier for silver polymeric membrane electrode was studied. The sensor gave a good Nernstian response of 58 +/- 1 mV per decade for silver ion in the activity range 3.3 x 10(-6) to 3.3 x 10(-2) M Ag+. The limit of detection reached 2.1 x 10(-6) M Ag+ and exhibited high selectivity for silver ion against the alkali, alkaline earth and transition metal ions. The sensor can be used in wide pH range from 1.5 to 6.5. The response time of the sensor is less than 20 s. The potentiometric sensor was used as the indicator electrode in the titration of Ag+ ions by sodium chloride solution. 相似文献
Curvature collineations are symmetry directions for the Riemann tensor, as isometries are for the metric tensor and Ricci collineations are for the Ricci tensor. Complete listings of many metrics possessing some minimal symmetry have been given for a number of symmetry groups for the latter two symmetries. It is shown that a claimed complete listing of cylindrically symmetric static metrics by their curvature collineations [1] was actually incomplete and is completed here. It turns out that in this complete list, unlike the previous claim, there are curvature collineations that are distinct from the set of isometries and of Ricci collineations. The physical interpretation of some of the metrics obtained is given. 相似文献
The equilibria between tungsten(VI) and iminodiacetic acid (IDA) have been studied in aqueous solution. The stoichiometry
and stability constants of the complexes formed are determined from a combination of potentiometric and Uv spectroscopic measurements.
All measurements are carried out at 25°C, pH 7.5 and different ionic strengths ranging from (0.1 to 1.0) mol dm−3 (NaClO4). According to these results, tungsten(VI) forms a mononuclear complex with IDA of the type (WO3L2−). By introducing two empirical parameters C and D in the complex-formation reaction between tungsten(VI) and IDA, the dependence
of the dissociation and stability constants on ionic strength is described by a modified Debye-Huckel-type equation. Finally,
a pattern for the ionic strength dependence is obtained. 相似文献
Infrared fluorescence observed after exciting to ν6 (ν=1) of CD3H with a Q-switched CO2 laser yields the exponential deactivation rate constant of 0.84 ms?1 torr?1. Rate constants for deactivation of CD3H by rare gases vary from 1.4 (for He) to 0.029 (for Xe) ms?1 torr?1. 相似文献
A generalisation of Carter's Circular metrics has been used for working out N potentials. It is pointed out here that the conformal extension of these metrics has the interesting property that the conformal time-like Killing vector depends only on time.
Zusammenfassung Bekanntlich existieren Raum-Zeit-Mannigfaltigkeiten, welche keine zeitartige Isometrie zulassen. In der vorliegenden Arbeit wird gezeigt: Falls die Metriken diese Raum-Zeit-Mannigfaltigkeiten als spezielle Verallgemeinerung der Carterschen zirkularen Metriken so gewählt werden, daß sie einen konformen zeitartigen Killing-Vektor zulassen, dann hängt dieser Vektor nur von der Zeit ab.
Rapid, selective collision-dependent excitation of N2O following pumping of SF6 with a CO2 laser is reported. The N2O fluorescence rise depends on the pressure of each component and is dominated by the SF6-dependent contribution of 2290 ms?1 Torr?1. The subsequent fall is governed by V→V processes among SF6 vibrational modes. 相似文献
A variety of alcoholic TBDMS (t-butyldimethylsilyl) ethers are easily removed in excellent yields by treatment with a catalytic amount of N-iodosuccinimide (NIS, 5 mol %) in methanol. This method is able to deprotect TBDMS ethers of alcohols in the presence of TBDMS ethers of phenols. 相似文献
Photocatalysis has been known as one of the promising technologies due to its eco-friendly nature. However, the potential application of many photocatalysts is limited owing to their large bandgaps and inefficient use of the solar spectrum. One strategy to overcome this problem is to combine the advantages of heteroatom-containing supports with active metal centers to accurately adjust the structural parameters. Metal nanoparticles (MNPs) and single atom catalysts (SACs) are excellent candidates due to their distinctive coordination environment which enhances photocatalytic activity. Metal-organic frameworks (MOFs), covalent organic frameworks (COFs) and carbon nitride (g-C3N4) have shown great potential as catalyst support for SACs and MNPs. The numerous combinations of organic linkers with various heteroatoms and metal ions provide unique structural characteristics to achieve advanced materials. This review describes the recent advancement of the modified MOFs, COFs and g-C3N4 with SACs and NPs for enhanced photocatalytic applications with emphasis on environmental remediation. 相似文献