A series of 5-chloro-N-aryl-1H-indole-2-carboxamide derivatives were prepared and evaluated as inhibitors of human liver glycogen phosphorylase a (hLGPa). One compound, 5-chloro-N-[4-(1,2-dihydroxyethyl)phenyl]-1H-indole-2-carboxamide (2f), inhibited hLGPa with an IC50 of 0.90 μM. The pyridine ...
The molecular conformation of achatin-II neutral form (H-Gly-Phe-Ala-Asp-OH), an endogenous peptide from the Achatina fulica ganglia, was elucidated by X-ray crystal analysis. The molecule takes an extended β-pleated structure stabilized by 5 intermolecular hydrogen bonds with the antiparallely...
3-Chloro-2-phenyl-isoindole-1-carbaldehyde has been prepared from N-phenylisoindolinone under Vilsmeier–Hack conditions. This electrophilic isoindole proved to be stable under the basic conditions used in the final treatment (KOH/MeOH), and for weeks under air in the solid state. Nevertheless, ...
Eight derivatives of N-(3-chloro-4-fluorophenyl)-2-(5-((3-(4-hydroxy-2, 2-dimethyl l-2,3-dihydrobenzofuran-5-yl)-1-phenyl-1H-pyrazol-4-yl)methylene)-4-oxo-2-thioxothiazolidin-3-yl) acetamide were synthesized by reacting pyrazole having substitutions at 1 and 3 positions (phenyl and benzofuran) w...
Crystals of new heterocyclic azo compound of 4-aminoantipyrine, 4-[(E)-(3-chloro-4-hydroxyphenyl)diazenyl]-1,5-dimethyl-2-phenyl-1,2-dihydro-3H-pyrazol-3-one have been grown by slow evaporation method at room temperature and its structural characterization was performed by X- ray diffraction met...
Two pyridazine derivatives, namely, 6-phenyl-3(2H)-pyridazinone (P1) and 3-chloro-6-phenylpyrazine (P2) were investigated for their influence on mild steel corrosion in 0.5 M HCl, using Tafel polarization, electrochemical impedance spectroscopy (EIS), surface morphology, FTIR and UV–vis techniq...
1.Lipid peroxidation in rat brain slices was induced by Fe+3/ascorbate.2.Brain lipid peroxidation, as measured by malondialdehyde formation, was inhibited by all the tested nitro aryl 1,4-dihydropyridine derivatives over a wide range of concentrations. The time-course antioxidant effects of the ...
Modifier-mixing provides a useful tool for tailoring the structural dynamics of oxide glasses. Its physical basis, however, remains subject to intense discussion. Here, we extend our previous consideration of Ca-Mg mixing in alkaline earth metaphosphate glasses [J. Non-Cryst. Solids 468, 74–81 ...
The viscosity and the shear relaxation behavior of supercooled Ag- and Sn- metaphosphate liquids are measured using parallel plate techniques. The fragility index m of these liquids, when taken together with that of other metaphosphate liquids, shows variation over a rather large range spanning ...
A new assay method is described for the simultaneous determination of free 3-methoxy-4-hydroxymandelic acid and 3-methoxy-4-hydroxyphenylethyleneglycol in plasma utilizing separation and purification by Bio-Gel P-10 followed by high-performance liquid chromatography with electrochemical detectio...
Urinary 3-methoxy-4-hydroxymandelic acid was low in 19 children with rheumatic fever and other collagen diseases as compared to 16 controls; its immediate precursors, the meta-catecholamines, were low too, though in a less pronounced way.The excretion of 3-methoxy-4-hydroxymandelic acid was plot...
Mandelic acid (MA) and 4-hydroxymandelic acid (HMA) are valuable specialty chemicals used as precursors for flavors as well as for cosmetic and pharmaceutical purposes. Today they are mainly synthesized chemically. Their synthesis through microbial fermentation would allow for environmentally su...
A specific method is described for the quantitative determination of 3-methoxy-4-hydroxymandelic (MOMA) acid in normal urine as well as in patients with pheochromocytoma. The procedure includes extraction of the acid from urine, followed by treatment of the extract with periodate to form vanilli...
Adsorptive-catalytic stripping voltammetry is commonly used for monitoring trace metals. This study reverses the scheme by developing a sensitive procedure for measuring the catalyst. The catalytic action of bromate upon the cathodic response of the adsorbed molybdenum-3-methoxy-4-hydroxymandeli...
The most important industrial process for the synthesis of vanillin is performed in two steps involving an condensation reaction of glyoxalic acid with guaiacol followed by an oxidative decarboxylation of the intermediary 3-methoxy-4-hydroxymandelic acid (MHPA) formed, thereby producing not only...
To analyze translesion DNA synthesis (TLS) across lesions derived from the air pollutant 3-nitrobenzanthrone in Escherichia coli, we constructed site-specifically modified plasmids containing single molecule adducts derived from 3-nitrobenzanthrone. For this experiment, we adopted a modified ver...
3-Nitrobenzanthrone (3-nitro-7H-benz[d,e]anthracen-7-one, 3-NBA) is a potent environmental mutagen that is found in diesel exhaust fumes and airborne particulates. It is known to produce several DNA adducts, including three major adducts N-(2′-deoxyguanosin-8-yl)-3-aminobenzanthrone (dG-C8-N-AB...
A sensitive method for determining 3-nitrobenzanthrone in surface soil was developed. 3-Nitrobenzanthrone was reduced to 3-aminobenzanthrone by refluxing at 60 °C with hydrazine and Raney nickel for 20 min, and 3-aminobenzanthrone was determined by normal-phase high-performance liquid chromatog...
The environmental contaminant 3-nitrobenzanthrone (3-nitro-7H-benz[d,e]anthracen-7-one) was recently shown to be a very strong bacterial mutagen, suggesting a new class of mutagenic compounds present in airborne particulate matter and diesel exhaust. Using the 32P-postlabeling assay, we investig...
2-Nitrobenzanthrone (2NB) was synthesized by reaction of N2O5 in CCl4 at room temperature and used to determine that the hydroxyl-radical- and nitrate-radical-initiated reactions of gas-phase benzanthrone (Bz) produced 2NB rather than 3-nitrobenzanthrone (3NB), the powerful bacterial mutagen fir...
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