A bioanalytical LC–MS/MS method was developed and validated for the simultaneous quantification of capsaicin (CAPS) and dihydrocapsaicin (D-CAPS) in dermal microdialysis samples from rats. Capsaicinoids were separated by using a C18 column, with a mobile phase of water and acetonitrile, both wi...
The quantified emissions of polychlorinated dibenzo-p-dioxins and polychlorinated dibenzofuran (PCDD/Fs) have not yet been reported comprehensively with the whole gasifier system. In this study, the emission characteristics of PCDD/Fs concentration, toxicity equivalent quantity, reaction mechani...
Attempts were made to synthesize all polychlorinated dibenzo-p-dioxin isomers containing six to eight chlorine atoms by micro-scale pyrolysis of different polychlorophenates. Eight of the ten possible hexachlorodibenzo-p-dioxins, the two hepta- and the octachlorodibenzo-p-dioxin were observed an...
A single dose of 2,3,7,8-tetrachlorodibenzo-p-dioxin (TCDD), 2,3,7-tribromodibenzo-p-dioxin (2,3,7-TBDD), 1,2,3,7,8,9-hexachlorodibenzo-p-dioxin (1,2,3,7,8,9-HCDD), 1,2,4,6,7,9-hexachlorodibenzo-p-dioxin (1,2,4,6,7,9-HCDD), or 1,3,6,8-tetrachlorodibenzo-p-dioxin (1,3,6,8-TCDD) was given to male ...
Planar chloro aromatics usually adopt a sheet/ribbon based 4 Å short axis structure, but when the molecule has a significant permanent dipole moment, an inverted layer motif characterized by axis doubling is obtained. This is exemplified by the title compounds. The packing of several related der...
N-Substituted acrylamidines, a new class of acrylic monomers, have been prepared from acrylonitrile, an alkyl halide, a Lewis acid and an amine. The synthesis involves the aminolysis of an N-alkylacrylonitrilium salt with an aliphatic or an aromatic amine. Following this general scheme, 4 exampl...
Recently, a novel series of amidines has been described, exhibiting high NR2B-subtype selective N-methyl-D-aspartate (NMDA) antagonist activity with nanomolar or subnanomolar affinity. Within the styrylamidine subclass, (E)-N-(2-methoxybenzyl)-3-phenyl-acrylamidine (1), displayed the highest aff...
α-1,4-Polygalactosamine (PGA) purified from the culture fluid of Paecilomyces sp. I-1 strain and N-acetylated α-1,4-polygalactosamine (NAPGA) are chitosan- and chitin-like biodegradable, compatible α-1,4-linked polysaccharides, respectively. Partially N-acetylated PGA was found to show the st...
Kasugamycin is an aminoglycoside antibiotic originally isolated from Streptomyces kasugaensis, which has been widely used for the management of plant diseases. However, photo-thermal instability and low efficiency limit its application. Therefore, it is an urgent task to prevent unwanted loss of...
Lignite is difficult to degrade, thus stimulation of the autochthonous lignite microflora and introduction of additional microorganisms are required for lignite decomposition. Here, a packed bed reactor, filled with lignite samples from the Konin region (central Poland) was supplied continuously...
Pentopyranoside and 6-deoxyhexopyranosides, such as those from d-xylose, l-arabinose and l-fucose are components of natural products, oligosaccharides or polysaccharides. Lewis acid promoted anomerisation of some of their alkyl O- and S-glycopyranosides is reported here. SnCl4 was more successfu...
To improve the properties of cytotoxic triterpenoid acids 1–5, a large set of hydrophilic esters was synthesized. We choose betulinic acid (1), dihydrobetulinic acid (2), 21-oxoacid 3 along with highly active des-E lupane acids 4 and 5 as a model set of compounds for esterification of which the...
Six new diterpenoids of the rare phyllocladane (13β-kaurane) type have been isolated from Plectranthus ambiguus. Their structures were determined on the basis of their spectral properties and by correlation with 16R,17-dihydroxyphyllocladane-3-one (calliterpenone).
The pentacyclic triterpenoid maslinic acid (1) was bioconverted by Cunninghamella blakesleana CGMCC 3.910, four metabolites were obtained. On the basis of nuclear magnetic resonance and high-resolution mass spectral analyses, their structures were identified as 2α,3β,7β-trihydroxyolean-12-en-...
17a-Methoxycarbonyl- and 17a-carboxamido-d-homoestra-1,3,5(10),17-tetraene derivatives were synthesized by palladium-catalyzed carbonylation reactions of the corresponding 17a-iodo-d-homoestra-1,3,5(10),17-tetraene derivatives using methanol and various amines as O- and N-nucleophiles, respectiv...
The syntheses of three 17α-acetoxy-13β-ethyl-11β-aryl-18,19-dinorpregna-4,9-diene-3,20 diones from levonorgestrel are described. Despite their close structural similarity to the antiprogesterone CDB-2914, one of the compounds exhibits agonistic progestational activity, and the other two compo...
d-Secooximes were synthesized from the d-secoaldehydes in the 13β- and 13α-estrone series. The oximes were modified at three sites in the molecule: the oxime function was transformed into an oxime ether, oxime ester or nitrile group, the propenyl side-chain was saturated and the 3-benzyl ether...
The synthesis of a novel series of N-(5-amino-1-(4-methoxybenzyl)-1H-pyrazol-4-yl amide derivatives 6a–o, 7a–s and their antiproliferative activities against A375P melanoma cell line were described. Most compounds showed competitive antiproliferative activities to sorafenib, the reference stan...
The reactions of the Cl radical with 1-butene and isobutene have been studied in a flow tube by utilizing photoionization mass spectrometry at the energy range of 9–11 eV. The addition C4H7Cl and abstraction C4H7 and C4H6 products were observed in the mass spectra. The experimental ionization e...
Enantiomerically pure tetrahydro-5-oxo-2-furancarboxylic esters can be prepared either by enzymatic resolution of the racemic γ-lactones themselves or by bioreduction with baker's yeast of dialkyl 2-oxoglutarates and subsequent cyclization of the resulting dialkyl 2-hydroxyglutarates. The ...
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