This paper reports the use of trifluoroacetic acid as a catalyst in the Dakin–West reaction for the synthesis of β-acetamido ketones. The method has several advantages such as requiring only mild conditions and a low concentration of catalyst. Screening of 19 β-acetamido ketones for antidiabe...

SnCl2·H2O has been found to be useful and highly efficient for the preparation of β-acetamido ketones and β-acetamido ketoesters by a one-pot reaction of aryl aldehydes, enolisable ketones, acetyl chloride and acetonitrile in a solvent-free media at room temperature. The present methodology o...

2,5-Diformylfuran (2,5-DFF) is an important furan-based chemical with broad application potential. To address the difficulties in isolating/purifying the product and recycling the 2,2,6,6- tetramethylpiperidine-1-oxy (TEMPO)-based catalysts, we employed a solvent with a low boiling point in whic...

Medically, bacterial ureases are important virulent factors and are used for treatment of peptic ulcers and urinary tones. Reported urease inhibitors are associated with various side effects including antibiotic resistance as a major one. Still there is an urgent need to synthesize new urease in...

New 17-picolyl and 17-picolinylidene androstane derivatives, 3–10, 15, 18, 19, 22 and 23, were synthesized starting from 17α-picolyl-androst-5-en-3β,17β-diol (1) and 17(Z)-picolinylidene-androst-5-en-3β-ol (2). Reaction of 1 with m-chloroperoxybenzoic acid gives 5α,6α-epoxy N-oxide deriva...

In liver homogenates from untreated rats the sulphur-substituted fatty acid analogues tetradecylthioacetic acid (CMTTD) was activated to its acyl-coenzyme A thioester. The activation was found to take place in the mitochondrial, microsomal and peroxisomal fractions. The activity of CMTTD-CoA syn...

Feeding tetradecyloxyacetic acid (a 3-oxa fatty acid) to rats led to decreased serum cholesterol and decreased serum triacylglycerol, resembling the effects of the corresponding 3-thia fatty acid (tetradecylthioacetic acid). The 3-oxa fatty acid inhibited strongly the mitochondrial fatty acid ox...

The influence of the peroxisomal proliferators perfluorooctanoic acid (PFOA), perfluorooctane sulphonic acid (PFOSA) and clofibric acid on lipid metabolism in rats was studied. Dietary treatment of male Wistar rats with these three compounds resulted in rapid and pronounced reduction in both cho...

(1) The activities of peroxisomal β-oxidation and palmitoyl-CoA hydrolase in Morris hepatoma 7800 C1 cells were studied. The cells were grown until they reached steady state (constant DNA content per dish) and then were cultured in the presence of fatty acids or alkylthioacetic acids, i.e., S-s...

[1-14C]odecylthioacetic acid (DTA), a 3-thia fatty acid, is ω (ω-1)-hydroxylated and sulfur oxygenated at about equal rates in rat liver microsomes. In prolonged incubations DTA is converted to (ω-hydroxydodecylsulfoxyacetic acid. ω-Hydroxylation of DTA is catalysed by cytochrome P450IVA1 (o...

Incorporation of thia fatty acids and their effects on the fatty acid composition in phospholipids has been investigated in 7800 C1 hepatoma cells and cultured hepatocytes. 3-Thia fatty acids of chain lengths from dodecyl- to hexadecyl-thioacetic acid were incorporated into phospholipids during ...

A single oral dose of two 3-thia (3-thiadicarboxylic and tetradecylthioacetic acids) and of 4-thia (tetradecylthiopropionic acid) fatty acids were administered to normolipidemic rats and their effects on lipid metabolism over a 24 hr period were studied. All three thia fatty acids could be detec...

Bis-(2-oxo-2-phenyl ethyl) tetrahydrofurfuryl phosphate (7) was synthesized by the addition of tetrahydrofurfuryl alcohol to the corresponding bis-ketol hydrogen phosphate (8) using DCC as the condensing agent. The rate of loss of a single ketol group was determined over the pH range 6.9 to 9 an...

Impaired energy metabolism is considered a possible cause of fatigue. The thiamine derivative, thiamine tetrahydrofurfuryl disulfide (TTFD), is prescribed and is also an over-the-counter drug for the attenuation of fatigue. It is readily absorbed from the intestinal tract and converted into thia...

Products of the interaction of 3,5-dinitrosubstituted ortho- and para-hydroxypyridines with [O(AuPPh3)3][BF4] are investigated by X-ray crystallography, IR and UV spectroscopy. The structure of the parent organic molecules are investigated by the spectroscopic methods and ab initio quantum chemi...

A new, highly stereoselective synthesis of (E)-droloxifene is reported. Deprotection of 3,4′-dimethoxybenzophenone and selective pivaloylation of the 3′-phenolic position gave 4-hydroxy-3′-(trimethylacetoxy)benzophenone. A McMurry reaction between the preceding benzophenone and propiophenone ...

The in vitro growth inhibitory activity of 26 thiazoles (including 4-halogeno-2,5-disubtituted-1,3-thiazoles) and 5 thienothiazoles was assessed on a panel of 6 human cancer cell lines, including glioma cell lines. (4-Chloro-2-(piperidin-1-yl)thiazol-5-yl)(phenyl)methanone (12a) and (4-bromo-2-(...

An efficient 2,3-dichloro-5,6-dicyano-1,4-benzoquinone/tert-butyl nitrite-catalyzed aerobic oxidation of diarylmethane sp3 C–H bonds in the presence of acetic acid has been developed. Under the optimal reaction conditions, a number of diarylmethanes can be directly converted to their correspond...

The conductivity of tetramethylammonium fluoride tetrahydrate (TMAF4) has been studied by impedance spectroscopy in the temperature range 213–322 K. The response of the cell Au|TMAF4|Au is typical for a polycrystalline electrolyte between solid blocking electrodes and it is temperature dependen...

Electrochemical properties of polycrystalline gold electrode/tetramethylammonium hydroxide solution interface have been studied as function of concentration and temperature by cycling voltammetry and impedance spectroscopy. Interfacial impedance has constant phase element (CPE) character with pa...