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.
[5,10,15,20-Tetrakis(4-N,N-dimethylaminobenzene)porphyrinato]Mn(III) acetate (MnTDPAc) was applied as an ionophore for an iodide-selective PVC membrane electrode. The influences of the membrane composition, pH of the test solution and foreign ions on the electrode performance were investigated. The sensor exhibited not only excellent selectivity to iodide ion compared to Cl- and lipophilic anions such as ClO4- and salicylate, but also a Nernstian response with a slope of -59.4 +/- 1.2 mV per decade for iodide ions over a wide concentration range from 1.0 x 10(-2) to 7.5 x 10(-6) M at 25 degrees C. The potentiometric response was independent of the pH of the solution in the pH range of 2 - 8. The electrode could be used for at least 2 months without any considerable divergence in the potential. Good selectivity for iodide ion, a very short response time, simple preparation and relatively long-term stability were the silent characteristics of this electrode. It was successfully used as an indicator electrode in the potentiometric titration of iodide ions, and also in the determination of iodide from seawater samples and drug formulations. 相似文献
Laser light is used for two-step photoionization of Na2. the first step depends on the moleculer orientation, the second step doesnot. This yields a method for the analysis of molecular alignment. 相似文献
The influence of solvent properties on acidity constants of some newly synthesized 9,10-anthraquinone and 9-anthrone derivatives was studied in methanol-water mixtures in a composition range of 0.57 to 1.0 methanol mole fraction. The model was established by using both multiple linear regression and target factor analysis. Both methods revealed that the solvent polarity/polarizability parameter * is a major factor in controlling the acidity behavior of the anthraquinones and anthrones studied in binary methanol-water mixed solvents. A QSPR study was conducted to drive the relationships between the * coefficient s and the polarity/polarizability of molecules. Both dipole moment and polarizability were found to have a linear relationship with s. The results confirm that, in the dipolar protic solvents used, the dipole-dipole interaction (for neutral molecules) and the ion-dipole interaction (for ionized molecules) are the major factors controlling the acidity behavior of these compounds. 相似文献
Sodium-dicyclohexyl- 18-crown-6 complex cation was used as carrier for the uphill transport of zinc as Zn(SCN)42? complex anion. By using L-cysteine as a metal ion acceptor in the receiving phase at the optimized pH of 7.6, the amount of zinc transport through the liquid membrane after 90 min was 97.2 ± 1.0%. The selectivity and efficiency of zinc transport from aqueous solutions containing equimolar mixtures of Ag+, Cd2+ Co2+, Cu2+, Fe2+, Ni2+, Pb2+, Pd2+, Sr2+, Bi3+, Cr3+ and Fe3+ ions was investigated. In the presence of NH2OH.HCl as a suitable masking agent in the source phase, the interfering effect of Cu2+ and Pb2+ ions was diminished drastically. 相似文献
Tribromoisocyanuric acid (TBCA) and Oxone®‐MX systems were used as effective oxidizing agents for the oxidation of thiols to their corresponding disulfides under mild conditions at room temperature with good to excellent yields. 相似文献