10.1111/cbdd.13744
The research focuses on the design and development of novel thiazolidin-4-one-1,3,5-triazine derivatives as neuro-protective agents against cerebral ischemia reperfusion injury in mice. The study involves the synthesis of these hybrid compounds and评估 their in vitro inhibition of NF-κB transcriptional activity in LPS-stimulated RAW264.7 macrophage cells. The most potent inhibitor, compound 8k, was further evaluated in vivo using a middle cerebral artery occlusion (MCAO) mice model to assess its neuro-protective effects. The experiments analyzed inflammation markers (TNF-α, IL-β, IL-6), oxidative stress markers (SOD, GSH, MDA), apoptosis markers (Bcl-2, Bax, cleaved caspase-3), and NF-κB signaling. The analyses included luciferase assays, ELISA, western blot, and various histopathological and neurological assessments. The research utilized various reagents, cell cultures, animal models, and a suite of molecular biology and histological techniques to evaluate the efficacy of the synthesized compounds as potential neuro-protective agents.
10.1002/asia.201000733
The research focuses on the synthesis and characterization of two trinuclear zinc-based cyclohelicates, Zn–PDB and Zn–PMB, which are designed to act as optical receptors for glutathione (GSH). The study explores the host-guest interactions between these cyclohelicates and GSH, as well as its component amino acids. The experiments involved the preparation of the cyclohelicates by incorporating amide-containing tridentate chelators into meta-positions of a substituted phenyl ring, followed by the addition of zinc ions. The synthesized compounds were characterized using single-crystal structure analysis, spectroscopic titrations, UV/Vis absorption, NMR titrations, and fluorescent titrations. These analyses were employed to investigate the formation of macrocyclic helical structures in both solid state and solution, as well as to determine the interaction modes and complexation stoichiometry with GSH. The results indicated that the Glu residue of GSH was positioned within the cavity of the cyclohelical hosts, with specific interactions occurring between the COO? groups and metal ions, and the Cys moiety of GSH with the amide groups of the host through hydrogen-bonding interactions, leading to measurable spectral changes.
10.1021/ja312092x
The research investigates the mediation of nitrite reduction by a water-soluble ferriheme model, FeIII(TPPS), which facilitates oxygen atom transfer from inorganic nitrite to various substrates, including a water-soluble phosphine (tppts), dimethyl sulfide, and biological thiols like cysteine and glutathione. The study explores the formation of reactive intermediates like sulfenic acids and nitrosyl complexes, and the subsequent redox transformations leading to the formation of N2O and NO. The experiments involve the use of optical absorbance measurements, NMR spectroscopy, mass spectrometry, infrared spectroscopy, gas chromatography, and amperometric analysis to monitor reaction progress, identify products, and quantify the concentrations of reactive species. The research also employs DFT calculations to understand the effects of proximal ligands on the Fe?NO bond and the lability of nitric oxide from ferrous heme nitrosyls.
10.1039/c2dt32727a
This research details the synthesis and characterization of a series of metal-organic frameworks (MOFs) based on the 2-(m-methoxyphenyl)imidazole dicarboxylate ligand, m-H3MOPhIDC. The purpose of the study was to explore the coordination features of the imidazole dicarboxylate ligand and its influence on the assembly of MOFs with potential applications in gas storage, catalysis, and more. The researchers successfully synthesized seven coordination polymers with diverse structures ranging from one-dimensional chains to three-dimensional frameworks by controlling synthetic conditions such as solvent and pH values. The chemicals used in the process included the ligand m-H3MOPhIDC, various metal salts (Sr(NO3)2, Cd(NO3)2·4H2O, Cu(ClO4)2, and CoCl2·6H2O), auxiliary ligands (1,10-phenanthroline and 2,2'-bipyridine), and Et3N as a base. The conclusions highlighted the significant impact of reaction conditions, core metal ions, and auxiliary ligands on the structures of the resulting MOFs, and confirmed the versatility of the m-H3MOPhIDC ligand in constructing novel MOFs with interesting structures and properties.
10.1039/c2ob25229e
The research focuses on the exploration of the trifluoromenadione core as a template for designing antimalarial redox-active agents that interact with glutathione reductase. The study involves the synthesis, electrochemical analysis, enzyme kinetics, and antimalarial activities of a series of 1,4-naphthoquinone derivatives, specifically focusing on their reactivity under quasi-physiological conditions in NADPH-dependent glutathione reductase reactions. The experiments utilized various reactants, including menadione, its fluoro-analogues, and atovaquone derivatives, and employed techniques such as cyclic voltammetry, enzyme assays involving human and Plasmodium falciparum glutathione reductases, mass spectrometry, and in vitro parasite cultures for assessing antiparasitic and cytotoxic effects. The analyses encompassed the determination of IC50 values, redox potentials, enzyme inhibition properties, and the chemical stability of the synthesized compounds. The research aimed to develop multitarget-directed drugs by combining the trifluoromenadione core with the alkyl chain of the antimalarial drug atovaquone, revealing a mechanism for the CF3 group as a leaving group and demonstrating potent antimalarial activity against malarial parasites in culture.
10.1016/j.tet.2012.09.020
The study investigates the role of steric and electronic effects on the antioxidant activity of tertiary amine-based diaryl diselenides, which mimic the function of glutathione peroxidase (GPx). The researchers synthesized various diselenides with methoxy substituents at different positions and evaluated their GPx-like activities using hydrogen peroxide, tert-butyl hydroperoxide, and cumene hydroperoxide as substrates, with thiophenol (PhSH) and glutathione (GSH) as co-substrates. The findings indicate that the position of the methoxy substituent significantly influences the catalytic activity. Specifically, the 6-methoxy substituent provides steric protection, preventing undesired thiol exchange reactions and the formation of seleninic and selenonic acids, thereby enhancing GPx-like activity. In contrast, the 4-methoxy substituent enhances activity when GSH is used as the co-substrate, likely due to its electronic effects. The study provides insights into the design of more effective GPx mimics by understanding the impact of substituent positions on the catalytic cycle and reactivity of these compounds.
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