107070-69-9

A simple novel and an easy-to-synthesize fluorescent probe 1 for detection of Zn2+ based on 1-(4-amino-2-hydroxyphenyl)ethan-1-one was developed. Probe 1 exhibited an effectively selective and sensitive recognition towards Zn2+ over Cd2+ and other cations. The Job's plot and HRMS experiments reveal the formation of 1:1 binding stoichiometry between probe 1 and Zn2+. The association constant (K) of probe 1 with Zn2+ was calculated to be 7.998 × 104 M?1. The detection limit of probe 1 towards Zn2+ was calculated at very low concentration up to 46 nM. The perfect reversibility of probe 1 for sensing Zn2+ was also demonstrated. Detection mechanism of Zn2+ ion by probe 1 was suggested through the analytical tools like UV–vis, FESEM, TEM, 1H NMR titration and the DFT calculations experiments. More importantly, the fluorescence imaging in C6 cells suggested that simple sensor had great potential in the application of biological imaging.

A novel series of dimethylamino chalcone-O-alkylamines derivatives was designed and synthesized as multifunctional agents for the treatment of AD. All the target compounds exhibited significant abilities to inhibit and disaggregate Aβ aggregation, and acted as potential selective AChE inhibitors, biometal chelators and selective MAO-B inhibitors. Among these compounds, compound TM-6 showed the greatest inhibitory activity against self-induced Aβ aggregation (IC50 = 0.88 μM) and well disaggregation ability toward self-induced Aβ aggregation (95.1%, 25 μM), the TEM images, molecular docking study and molecular dynamics simulations provided reasonable explanation for its high efficiency, and it was also found to be a remarkable antioxidant (ORAC-FL values of 2.1eq.), the best AChE inhibitor (IC50 = 0.13 μM) and MAO-B inhibitor (IC50 = 1.0 μM), as well as a good neuroprotectant. UV–visual spectrometry and ThT fluorescence assay revealed that compound TM-6 was not only a good biometal chelator by inhibiting Cu2+-induced Aβ aggregation (95.3%, 25 μM) but also could disassemble the well-structured Aβ fibrils (88.1%, 25 μM). Further, TM-6 could cross the blood-brain barrier (BBB) in vitro. More importantly, compound TM-6 did not show any acute toxicity in mice at doses of up to 1000 mg/kg and improved scopolamine-induced memory impairment. Taken together, these data indicated that TM-6, an excellent balanced multifunctional inhibitor, was a potential lead compound for the treatment of AD.

Alzheimer's disease (AD) is associated with impaired Aβ degradation in the brain. Enhancing the process of Aβ clearance is an attractive potential AD therapy. Treatment with LXR agonists may reduce Aβ levels in vivo. However, the clinical potential of man

The carbonyl stretching frequencies of substituted 2-Me, 2,6-diMe, 2-MeO benzophenones and 2-Me, 2-MeO acetophenones have been measured in diluted CCl4 solutions.Two interaction mechanisms are observed.In X, Y substituted benzophenones with X on the same cycle as the ortho group and Y on the other cycle, it is shown that for X=Y, the effect of Y is greater than that of X except for very strong electron-releasing substituents.In this last case, the observed enhancement is attributed to the joint effects of intercycle interactions excercised on X and Y and of intracycle interaction on X.These results are corroborated by the study of substituted acetophenones in which only the intracycle mechanism can play a role.