PurposeFenfluramine is being developed as a low-dose adjunctive treatment for seizures in patients with Dravet syndrome and other epileptic encephalopathies, including Lennox-Gastaut syndrome. Most patients with Dravet syndrome receive multiple antiepileptic drugs, making it challenging for care...
Perivascular adipose tissue (PVAT) modulates vascular tone and altered PVAT function is observed in vascular diseases such as hypertension and atherosclerosis. We discovered that the PVAT surrounding rat thoracic aorta (RA) and the superior mesenteric artery (SMA) contain significant amounts of ...
1-Dimethylsilyl- and 1,3-bis(dimethylsilyl)adamantane have been prepared in low yield by Wurtz reaction of dimethylchlorosilane with 1-chloroadamantane or 1,3-dichloroadamantane, respectively. On the other hand, reaction of phenyldimethylsilyllithium with 1-bromoadamantane or 1,3-dibromoadamanta...
Oxygen-fuel combustion is a promising technology for CO2 emission reduction. The high-temperature entrained flow reactor and high-temperature drop tube furnace were used to analyses the formation and O2/CO2 combustion characteristics of real-environment coal char in high-temperature oxy-fuel con...
The study describes the synthesis of new β2,2-peptides made from geminally disubstituted β2,2-amino acid and their folding propensities. The (R)-C-linked carbo-β2,2-amino acid [(R)-β2,2-Caa] was prepared from d-glucose and converted into the homo-oligomeric di-, tetra-, and hexapeptides. The...
The interest in the study of heteroaromatic thioamides which are known to exhibit antithyroid activity is stimulated by the variety and an unusual structure their complexes with molecular iodine.The directions of dithiones investigation are diversity enough, however a few works are devoted to th...
A five-step total synthesis of aaptamine, 1a, is described starting from 6,7-dimethoxy-1-methylisoquinoline
In previous studies we identified several 1-aryl-6,7-dimethoxy-1,2,3,4-tetrahydroisoquinoline derivatives displaying potent anticonvulsant effects in different animal models of epilepsy. With the aim to deepen the structure–activity relationships (SAR) for this class of compounds and identify n...
1.1. Activity of S-adenosylmethionine decarboxylase, one of the rate-limiting enzymes of polyamine biosynthesis, was determined in oocysts of Eimeria stiedai, a coccidian parasite of the rabbit.2.2. Several properties of the enzyme were compared to the mammalian enzyme. It showed considerably le...
1. Two phenylated compounds of methylglyoxal bis(guanylhydrazone), potentially inhibitors of diamine oxidase activiy, have been synthesized: phenylglyoxal bis(guanylhydrazone) and diphenyl-glyoxal bis(guanylhydrazone).2. Their inhibitory capacity was tested: while PGBG was able to reduce the enz...
The 6-nitro- and 8-nitro- groups in the tetrazolo[1,5-a]pyridine molecule exhibit completely different influences on the tetrazole–azide equilibrium. Introduction of the methyl-, nitro-, azido groups or a bromine atom in positions 5, 6, 7 or 8 of the nitrotetrazolopyridine produce changes in th...
To search for new cruzain inhibitors, the synthesis of a series of novel 2-(N′-benzylidenehydrazino)-4-trifluoromethyl-pyrimidines in a convergent manner is presented. The cruzain inhibitory activity of some of these compounds was evaluated and a binding model was proposed. All derivatives test...
A series of novel 6,7-dihydro-5H-cyclopenta[d]pyrimidine derivatives was successfully designed, synthesized and evaluated as a new chemical scaffold with vascular endothelial growth factor receptor (VEGFR 2) inhibitory activity. Compounds 6c and 6b showed enzyme inhibition of 97% and 87% at 10 µ...
A water-soluble 4S,5S-derivative of heptaplatin, cis-{Pt(II)[(4S,5S)-4,5-bis(aminomethyl)-2-isopropyl-1,3-dioxolane]·(3-hydroxyl-cyclobutane-1,1-dicarboxylate)} was synthesized. The anticancer activity and toxicity were evaluated by comparing its interaction with DNA, cytotoxicity against four ...
A study was made on the effect of dithiothreitol (DTT; present during irradiation) on M1 ovule sterility, M2 embryonic lethals, M2 chlorophyll mutants and M2 viable mutants induced with fast neutrons or X-rays in Arabidopsis thaliana. DTT provides considerable protection against both fast-neutro...
Dithiothreitol was found to be a competitive inhibitor for a purified L-fucose isomerase from Aerobacteraerogenes, inhibiting enzyme activity for the isomerization of both L-fucose and D-arabinose. The kinetics of inhibition showed that the oxidized form was the more potent inhibitor. The Ki for...
The UV detection sensitivity of ZnO nanoparticles in capillary electrophoresis (CE) analysis was selectively enhanced, by 27 or 19 folds, after adsorption of dithiothreitol (DTT) or cysteine (Cys) in 10 mM sodium phosphate buffer. Adsorption equilibrium was reached within 90 min for DTT but only...
Tenderness, flavour, overall liking and odour are important components of sheepmeat eating quality. Consumer assessment of these attributes has been made for carcasses from the Information Nucleus Flock (INF) of the Cooperative Research Centre for Sheep Industry Innovation. The concentrations of...
Kinetics of miniemulsion polymerization of 1,6-hexanediol diacrylate (HDDA) was investigated. The particle size of microgel particles remained relatively constant (ca. 270 nm) during polymerization in the temperature range 65–75 °C. The model-fitting method in combination with the model-free m...
Electron beam curing of bisphenol A diglycidyl ether diacrylate resin (BDGDA) mixed with varying amount of 1,6-hexanediol diacrylate monomer (HDDA) was investigated using low energy DC electron beam accelerator. Cured coating films were analyzed by Fourier transformed infrared spectroscopy (FTIR...
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