Four isomeric chloro-substituted 2-methylbenzyl radicals were generated from the corona discharge of 3- and 4-chloro-o-xylenes seeded in a large amount of He carrier gas using a technique of corona excited supersonic expansion coupled with a pinhole-type glass nozzle. The observed visible vibron...
Different N,N-diacylaniline derivatives such as N-acetyl-N-(2-methoxyphenyl)acetamide, N-acetyl-N-(2-Methoxy-phenyl)-4-nitrobenzamide, N-(4-nitrobenzamide)-N-(2-Methoxy-phenyl)-4-bromobenzamide, N-Acetyl-4-nitro-N-o-tolyl-benzamide, N-Acetyl-N-o-tolyl-acetamide, and 2-Chloro-N-(2-chloro-acetyl)-...
The crystal and molecular structure of N-(4-chloro)benzoyl-N′-2-tolylthiourea (C15H13N2OSCl, Mr=304.79) is determined by X-ray diffraction. The crystal structure is monoclinic, space group P21/n with a=3.9898(3), b=22.922(2), c=16.005(2)Å, β=104.367(4)°, V=104.367(4)Å3, Z=4, Dc=1.428g/cm3. ...
A series of N-((1,3-diphenyl-1H-pyrazol-4-yl)methyl)aniline derivatives (5a–8d) have been designed and synthesized, and their biological activities were also evaluated as potential antitumor and cyclin dependent kinase 2 (CDK2) inhibitors. Among all the compounds, compound 5a displayed the most...
N-(Chloro-3-methoxyphenyl)-2-picolinamide (3, ML128, VU0361737) is an mGlu4 positive allosteric modulator (PAM), which is potent and centrally penetrating. 3 is also the first mGlu4 PAM to show efficacy in a preclinical Parkinson disease model upon systemic dosing. As a noninvasive medical imagi...
Aldol condensation of acetaldehyde and benzaldehyde with the lithium ester enolate of ethyl N,N-dimethylglycine in the presence of one equivalent of triethylborane resulted in the formation of the corresponding 3-hydroxy-2-amino acid ester with excellent stereocontrol (>95% de ) for the formatio...
The synthesis and characterization of aminoacetyl cellulose and thioacetyl cellulose is presented in this paper. Cellulose was first chemically modified with chloroacetyl chloride using N,N-dimethylformamide (DMF) as reaction medium. The maximum substitution of hydroxyl groups of cellulose was a...
3,5-Bis-(trifluoromethyl)phenyl isothiocyanate, was used as a convenient reagent for the derivatization of histamine, tyramine, tryptamine and 2-phenylethylamine, which eliminates the purification step. The obtained derivatives were determined by liquid chromatography-tandem mass spectrometry (L...
Ko143, a potent ABCG2 inhibitor that reverses multidrug resistance, cannot be used clinically due to its unsuitable metabolic stability. We identified benzoyl indoles as reversal agents that reversed ABCG2-mediated multidrug resistance (MDR), with synthetic tractability and enhanced metabolic st...
Nitrated polycyclic aromatic hydrocarbons are more mutagenic and carcinogenic than parent PAHs. The formation mechanism of dinitro-pyrenes initiated by OH from mononitro-pyrenes was conducted by quantum chemical calculations. The products are 1,2-, 1,7-, 2,4-, 2,5- and 2,7- dinitropyrenes. Water...
Mycobacterial glycopeptidolipid (GPL) interactions with membranes were analysed with monolayer experiment, using GPLs bearing 3, 1, or 0 carbohydrate residues (GPL3, GPL1, GPL0). Compression isotherms and surface potential determinations suggested that the glycopeptidic moiety of GPL3 permanentl...
The synthesis of thieno[3,2-b]pyridines was achieved using a three-step process allowing the construction of the thiophenic ring with 17–34% overall yields. The key step was the regioselective lithiation–bromination of the 3-methylthiopyridine induced by BuLi–LiDMAE superbase followed by Sono...
O-Polysaccharides were isolated by mild acid degradation of the lipopolysaccharides of Escherichia coli O123 and Salmonella enterica O58 and studied by chemical methods and 2D 1H and 13C NMR spectroscopy, including experiments in a H2O/D2O mixture, which enabled observation of correlations for n...
The O-specific polysaccharide was isolated from the lipopolysaccharide of type strain Idiomarina abyssalis КММ 227T and studied by sugar analysis, Smith degradation, and two-dimensional 1H and 13C NMR spectroscopy including 1H,1H-TOCSY, 1H,1H-COSY, 1H,1H-ROESY, 1H,13C-HSQC, 1H,13C-HMBC, 1H,13...
Insoluble poly(vinyl benzyltriphenylphosphonium dichromate) reagent was prepared by chemical modification of 2% crosslinked polychloromethylstyrene with triphenylphosphine, followed by treatment of the obtained polymeric salt with chromium trioxide in water. The activity of the resulting polymer...
Temperature extremes represent an important limiting factor to plant growth and productivity. Low concentration of hydrogen sulfide (H2S) has been proven to function in physiological responses to various stresses. The present study evaluated the effect of foliar application of wheat seedlings wi...
Thioglycine and l-thiovaline are stable under acidic and basic conditions but in the presence of bicarbonate they liberate the gasotransmitter H2S. In cells both thioamino acids were proven to enhance cGMP formation and promote vasorelaxation in mouse aortic rings. Given that H2S is known to low...
H2S donors are substitutes of H2S with various biological activities like inhibiting the inflammatory response and protecting myocardial cells from injury. In order to confirm whether the H2S donors have drug-like properties, two series thiophosphamide H2S donors were evaluated including toxicit...
Phenolic compounds in fruit are involved in responses to biotic and abiotic stresses and are responsible for organoleptic properties. To establish the distribution of these secondary metabolites at the tissue and sub-cellular scales, mapping of fluorescence in apple epidermis and outer cortex ti...
A cascade operation was designed to synthesize nine coumarin-substituted dihydropyrazoles with only one or two phenolic hydroxyl groups contained. Antioxidant abilities of the obtained compounds were evaluated by inhibiting 2,2′-azobis(2-amidinopropanehydrochloride) (AAPH)-, Cu2+/glutathione (G...
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