10.2174/157017811799304098
The research focuses on the efficient synthesis of 1,4-disubstituted piperazine-2,5-diones, which are significant as biologically active natural products and important in drug discovery. The study developed a simple and efficient method for their synthesis using potassium iodide catalysis in aqueous media, specifically in an acetone/water mixture. The reactants used were N-substituted chloroacetamides, potassium carbonate as a base, and potassium iodide as a catalyst. The experiments involved refluxing these reactants and optimizing conditions to achieve high yields of the desired piperazinediones. The structures of the synthesized products were confirmed through elemental analyses, infrared (IR), proton (1H) and carbon-13 (13C) nuclear magnetic resonance (NMR) spectroscopy, and in some cases, single crystal X-ray diffraction analysis. The article also discusses the influence of solubility and steric hindrance on the reaction yields and mentions ongoing investigations into the biological activities of these compounds.
10.1016/j.bmcl.2012.04.068
The research focuses on the development of fluorescent 2-styrylpyridazin-3(2H)-one derivatives as probes for detecting amyloid-beta (Ab) plaques in Alzheimer's disease (AD). The study evaluates 28 synthesized compounds, which are created through a series of chemical reactions involving reagents such as potassium iodide, triphenylphosphine, and benzaldehyde. Compound 9n emerges as the most promising, exhibiting a significant increase in fluorescence intensity (FAb/F0 = 40.84) and high binding affinity (Kd = 1.84 μM) to Ab aggregates. This compound is tested for its ability to stain intracellular Ab aggregates in SHSY5Y neuroblastoma cells and Ab plaques in brain sections from transgenic AD model mice (APP/PS1), showing consistent results with thioflavin T staining. The findings suggest that 2-styrylpyridazin-3(2H)-one derivatives, particularly compound 9n, could serve as effective fluorescent imaging agents for studying AD.
Xn,
Xi,
N
