Two emerging psychoactive substances, 2-(2,5-dimethoxy-4-methylphenyl)-N-(2-methoxybenzyl)ethanamine (25D-NBOMe) and N-(2-methoxybenzyl)-2,5-dimethoxy-4-chlorophenethylamine (25C-NBOMe), are being abused, leading to fatal and non-fatal intoxications. However, most of their adverse effects have b...
Bis(2,4,6-trimethylphenyl)chlorobismuth (1), synthesized by comproportionation reaction of tris(2,4,6-trimethylphenyl)bismuth and bismuth chloride, was reduced with sodium in liquid ammonia. By subsequent insertion of oxygen into the Bi–Bi bond of the intermediate dimer tetrakis(2,4,6,-trimethy...
The present study was undertaken in order to rationalise the apparent biological inactivity of 15,16-dihydro-6- methylcyclopenta[a]phenanthren-17-one (4) when other methyl isomers of 15,16-dihydrocyclopenta[a]phenanthren-17- one e.g. the 11-methyl derivative (2), display appreciable tumorigenici...
A series of four 11-alkoxy cyclopenta[a]phenanthren-l7-ones, ranging from the methoxy to the butoxy derivative, has been synthesised in order to investigate the effect of the size of the 11-substituent on the mutagenicity and ability of these compounds to induce hepatic CYP1 activity in rats. Th...
The in vitro metabolism and activation to mutagens of 15,16-dihydrocyclopenta[a]phenanthren-17-one (CPP-17-one) were investigated using hepatic preparations from rats pretreated with prototype inducers of the cytochrome P-450-dependent mixed-function oxidases. Aroclor 1254-induced microsomes wer...
Extraction procedure and detection of bis(2-chloroethyl)sulfide from urine samples of two patients are described using gas chromatography-mass spectrometry. Concentrations are found in the low ppb-range. The result is discussed in connection with the reactivity of this substance and the correspo...
Modified gold electrodes have been used for the in situ electrocatalytic oxidation of blister agent simulant 2-choloroethyl ethyl sulfide (CEES). The preparation of composite film based on copper phthalocyanine (CuPc) and air and water stable room temperature ionic liquid (RTIL) 1-butyl-3 methyl...
Series of V2O5–TiO2 catalysts with varying vanadium content are prepared by impregnation method. The catalyst composition is determined by XRD and Smart mapping (SEM–EDAX), respectively. The bulk reducibility of the catalyst is determined by the temperature programmed reduction (TPR). Catalyst...
The decontamination of surfaces exposed to chemical warfare agents is an interesting scientific topic. The desorption behavior of bis(2-chloroethyl) sulfide (sulfur mustard, HD) from the surface of the HD-contaminated hardened cement paste (HCP) was investigated under different weather condition...
Zinc oxide nanocubes were surveyed for their destructive turn-over to decontaminate 2-chloro ethyl phenyl sulfide, a sulfur mustard simulant. Prior to the reaction, nanocubes were prepared through sol-gel method using monoethanolamine, diethylene glycol, and anhydrous citric acid as the stabiliz...
Bis(2-chloroethyl) ether (BCEE) is a common chemical material and a frequently detected contaminant in groundwater. It has a strong toxicity and some other chemicals such as poly(vinyl chloride-co-isobutyl vinyl ether) contain similar chloroaliphatic ether structure. So the effective degradation...
Oxidative stress is the major mechanism impairing cell homeostasis, inducing cell death and tissue damage in sulfur mustard (SM)-exposed individuals. The aim of the present study was to evaluate time course changes of oxidative stress in the mice exposed with 2‑chloroethyl ethyl sulfide (CEES) a...
The cytotoxic effects and alkylating activity of a series of 3-[1-(alkylamino)-ethylidene]-chroman-2,4-dione (4a–4c), 2-methoxy-3-[1-(alkylamino)-ethylidene]-2,3-dihydro-2,4-dioxo-2λ5-benzo[e][1,2] oxaphosphinane (5a–5c) and [2-oxo-4-phenyl(alkyl)-2H-chromen-3-yl]-phosphonic acids dimethyl es...
N-Alkyl-N-benzyloxy carbamates, 2, undergo facile intramolecular cyclization with a variety of carbon nucleophiles to give functionalized five- and six-membered protected cyclic hydroxamic acids, 3, in good to excellent yields. This method can be extended to prepare seven-membered cyclic hydroxa...
We described in this paper an efficient synthesis of variously substituted 4-phosphinoyl-4,5,6,7-tetrahydro-2H-indazol-3-ylamines involving nucleophilic addition of hydrazine on β-ketothioamides as key-step.
Palladium catalyzed cross-coupling of 3-amino- and 3-acylamido-2-bromopyridines 1a–f with triethyl phosphite allowed the synthesis of 3-amino- and 3-acylamido pyridine-2-phosphonic acid diethyl esters 2a–f, whereas nickel catalysts, although providing access to related anilido-2-phosphonates, ...
The behaviour at HMDE and SMDE of 8-hydroxy-7-(4-sulfo-1-naphthylazo)-5-quinolinesulfonic acid has been studied by several techniques including Square wave voltammetry (SWV), Differential pulse plarography (DPP), Direct current polarography (DCP) and Cyclic voltammetry (CV). Current–potential c...
Based on 1,4-diarylpiperidine-4-methylureas, a new class of ACAT inhibitors, we examined in the study the SAR of a series of compounds prepared by replacing the substituent at the three aromatic parts. Introduction of long alkoxy group onto the phenyl moiety at the B-part was effective in improv...
BackgroundCryopyrin associated periodic syndromes (CAPS) are a group of autoinflammatory diseases linked to gain-of-function mutations in the NLRP3 gene which cause uncontrolled IL-1β secretion. Proton pump inhibitors (PPIs), commonly used as inhibitors of gastric acid production, also display ...
Cholangiocarcinoma is one of the deadliest malignancies worldwide. Recent studies reported that treatment with gemcitabine was effective in prolonging survival. However, as the treatment only benefited a limited subset of patients, selection of patients before treatment is required. To discover ...
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