The mid- and near-infrared spectra of hydrogen bond complexes between phenol derivatives and N,N-dimethylformamide are investigated. The enthalpies of complex formation determined in carbon tetrachloride range from 23 to 26.6 kJ mol−1. Some spectroscopic features observed in the mid- and near-in...

The hydrogen bond complexes between phenol derivatives (pKa = 10.20−8.20) and N-methyldiacetamide (NMD) are studied by mid- and near-IR spectroscopy in carbon tetrachloride solution. The equilibrium constants and enthalpies of complex formation are determined and the results suggest that the pro...

The reaction of N-(3,4-dichlorophenethyl)-N-methylamine (1) with 3-chloromethyl-5-phenyl-1,2,4-oxadiazole (2) was investigated. Employment of an equimolar amount of 1 and 2 in the presence of potassium carbonate led to the expected tertiary amine 3 (N-[(3,4-dichlorophenyl)ethyl]-N-methyl-N-[(5-p...

3-Bromopyruvic acid has been shown to be a highly effective growth inhibitor of certain yeasts. Wide differences were noted in the inhibitory activity of the compound among different species and genera of yeast.

AimsCancer cells, due to the Warburg effect, are more dependent on glycolysis than normal cells, so glycolytic inhibitor 3-bromopyruvic acid (3-BP) was proposed as a promising candidate for anticancer therapy. Overexpression of multidrug transporters is the main reason of resistance of cancer ce...

Background3-Bromopyruvic acid (3-BP), a glycolytic inhibitor and a promising anticancer compound, induces oxidative stress and depletes cells of glutathione (GSH). The causes of GSH loss remain unclear. The aim of this study was to ascertain whether 3-BP forms a conjugate with glutathione.

Aims3-Bromopyruvate (3-BP), an alkylating agent and a glycolytic inhibitor, is a promising anticancer agent, which can be efficient also against multidrug-resistant cancer cells. The aim of this study was to examine how 3-BP affects the survival and mobility of rat (MAT-LyLu and AT-2) and human ...

In this work, a series of 2-substituted-thio-N-(4-substituted-thiazol/1H-imidazol-2-yl)acetamide derivatives were developed as β-secretase (BACE-1) inhibitors. Supported by docking study, a small library of derivatives were designed, synthesized and biologically evaluated in vitro. In addition,...

The Ugi three-component reaction with 2-substituted five-, six-, and seven-membered cyclic imines was investigated. The reaction opens a new route to substituted proline and homoproline derivatives. It was shown that the method is efficient for the one-step preparation of seminatural dipeptides ...

The pivaloyloxyethyl ester of methyldopa is an antihypertensive prodrug possessing improved bioavailability properties over methyldopa. A sensitive cation-exchange, high-performance liquid chromatographic assay using electrochemical detection has been developed for the ester in plasma and urine ...

The effect of l-penicillamine administration on rat liver transaminase activities and on the excretion of vitamin B6 activity in the urine was investigated. l-Penicillamine caused a reduced activity of the alanine-glutamic and aspartic-glutamic transaminases. Reversal of the inhibition was accom...

Previous studies have shown that cysteine and penicillamine induce gene mutations in Salmonella typhimurium, the effect being strongly potentiated in the presence of mammalian tissue preparations. It has now been demonstrated that homogenate of V79 Chinese hamster cells is an efficient activator...

By comparing the effect of two nitric oxide (NO)-containing compounds, we found that S-nitroso-N-acetyl-d,l-penicillamine (SNAP), but not GEA 3175 (1,2,3,4-Oxatriazolium,3-(3-chloro-2-metylphenyl)-5-[[(4-methylphenyl)sulfonyl]amino]-, hydroxide inner salt), released NO. Despite this, both drugs ...

A method for a fast quantitative determination of the l-isomer in d-penicillamine is described. l-Leucine is coupled to d,l-penicillamine and the resulting diastereomers separated by reversed phase liquid chromatography. The mild conditions for the derivatization cause no racemization. For detec...

In soluble fractions prepared from rat liver homogenates, l-penicillamine hydantoin appeared to be, on the basis of SH consumption measurements, a substrate for glutathione peroxidase but not transferase reactions. When glutathione is incubated with rat liver soluble proteins in the presence of ...

l-[14C]Penicillamine is bound to RNA from rat liver in an in vitro reaction catalyzed by rat liver aminoacyl-tRNA synthetases. Addition of certain naturally occuring amino acids results in a significant decrease of l-penicillamine binding. The most potent inhibitor of this binding is l-valine, f...

SummaryL-Penicillamine is taken up and accumulated by mammalian cells via their amino acid transport systems. Natural amino acids compete with L-penicillamine and have a higher affinity to their transport systems, as shown in the case of L-valine.D-Penicillamine is not accumulated within the cel...

A new HPLC method by fluorescence or UV/vis absorbance detection has been developed for the separation and quantification of penicillamine stereoisomers after their spirocyclization with ninhydrin. The separation was performed on an achiral C18 column by isocratic elution with a copper(II)-l-pro...

An unusual reaction involving ninhydrin and aminothiols was exploited to set an indirect method for the chiral recognition of stereoisomers of penicillamine. Separation of diastereoisomers was achieved on a C18 column in isocratic mode by using a mixture of propionic acid (pH 3.0)/acetonitrile/w...

d-Penicillamine derived thiazolidine ligands were prepared in a two-step synthetic sequence and used in the enantioselective alkylation of a variety of aromatic aldehydes with diethylzinc at room temperature. Excellent ee, up to >99%, and nearly complete conversions were observed. Structurally a...