Effects of the 5-hydroxytryptamine (5-HT)1A/1B/2C receptor agonist N-[3-(trifluoromethyl)phenyl] piperazine (TFMPP, 0–3.0 mg/kg s.c.) and the 5-HT2C receptor agonist 8,9-dichloro-2,3,4,4a-tetrahydro-1H-pyrazino[1,2-a]quinoxalin-5(6H)-one (WAY 161503, 0–3.0 mg/kg s.c.) in place conditioning wer...

A fruitful switch from tert-butyl to cumene hydroperoxide was able to overcome a difficulty arose in the enantioselective oxidation of fluorinated aryl benzyl sulfide with hydroperoxides in the presence of a titanium/(S, S)-hydrobenzoin catalyst. New experiments show the complementarity of the o...

This study reports an investigation of omeprazole and venlafaxine parent substances and metabolites in Italian municipal influent wastewaters (IWWs). These pharmaceuticals were selected because they are widely consumed in Italy, but are poorly detected in waste and surface water. The aim of the ...

Omeprazole is one of the world-wide most consumed pharmaceuticals for treatment of gastric diseases. As opposed to other frequently used pharmaceuticals, omeprazole is scarcely detected in urban wastewaters and environmental waters. This was corroborated in a previous research, where parent omep...

We report a novel method for the simultaneous determination of omeprazole and their main metabolites (omeprazole sulphide, omeprazole sulphone and 5-hydroxy omeprazole) in human urine samples. For this purpose, two new capillary electrophoresis (CE) methods were developed for the simultaneous de...

Cross-talk between nuclear receptors involved in the control of drug metabolism is being increasingly recognised as a source of drug side effects. Omeprazole is a well known activator of the aryl hydrocarbon receptor (AhR). We investigated the regulation of AhR by omeprazole-sulphide, a degradat...

Omeprazole is one of the world-wide most frequently prescribed and administered pharmaceuticals in humans for the relief of gastro-intestinal disorders. Despite its high worldwide consumption, omeprazole is rarely detected in urban wastewaters and environmental waters. On the other hand, its hum...

We report the syntheses of a single enantiomer of an unprotected ketomycolic acids containing a cis-cyclopropane and of related hydroxy-mycolic acids.

The exchange of tritium from meso-2,3-ditritiosuccinate and racemic-2-tritiosuccinate to water was studied using soluble and particulate preparations of succinic dehydrogenase from heart muscle. All the tritium exchanges. We conclude from kinetics that the enzyme fails to discriminate strongly a...

The distribution of hydrogen isotope between pro-R and pro-S positions of succinic acid has been determined by comparison of its isotopic content before and after incubation with isocitrate lyase. This enzyme, in the presence of glyoxylate, exchanges exclusively the pro-S protons of succinate wi...

The aim of this study was to investigate the integration of nanofiltration in succinic acid production based on a fermentation. An experimental investigation was carried out with NF 45 membrane and synthetic fermentation broths of increasing complexity containing succinate salt and different imp...

Diethyl 2-alkyl-2-hydroxymalonates react with DAST almost exclusively at the ester carbonyl giving a mixture of ethyl 2-(ethoxydifluoromethyl)-2-hydroxyalkanoates, 1,1-bis(ethoxydifluoromethyl)alkan-1-ols when administered at room temperature in dichloromethane. The reaction was exploited in the...

New microtubule depolymerizing agents with potent cytotoxic activities have been prepared with a 5-cyano or 5-oximino group attached to a pyrrole core. The utilization of ortho activation of a bromopyrrole ester to facilitate successful Suzuki-Miyaura cross-coupling reactions was a key aspect of...

The reaction of [18F]fluoromethyl tosylate with methyl(tert-butoxycarbonyl)-l-tryptophanate results in formation the O-alkylated ester of the tryptophan instead of alkylation of the indole nitrogen of tryptophan as initially anticipated. Treatment of protected tryptophan with NaH in dimethyl for...

Inhibition data on rat monoamine oxidase B isoform of a large number of 7-metahalobenzyloxy-2H-chromen-2-one derivatives (67 compounds) carrying at position 4 a variety of substituents differing in steric, electrostatic, lipophilic and H-bonding properties, were modeled by Gaussian field-based 3...

(±)-N-Methyl-N-[trans-2-(1-pyrrolidinyl)cyclohexyl]-1-phenylcyclopropanecarboxylic amide (1) and its dichloro analog (2) were synthesized. Compounds 1 and 2 are related to the κ-selective opiate U-50488 in that the benzylic methylene moiety in U-50488 has been replaced by a cyclopropane ring. ...

Each of the four aromatic –CH= of (S,R)-2-pyrrolidinyl-1,4-benzodioxane [(S,R)-6] and of its epimer at the dioxane stereocenter (S,S)-6, previously reported as α4β2 nAChR ligands, was replaced with nitrogen. The resulting four diastereoisomeric pairs of pyrrolidinyl-pyridodioxanes were studie...

Here we demonstrate that the thiol-reactive, environmentally sensitive fluorogenic molecules 6-bromoacetyl-2-dimethylaminonaphthalene and 6-acryloyl-2-dimethylaminonaphthalene are substrates for glutathione transferases (GSTs). Product formation can be measured by strong increase in fluorescence...

Fatty acid synthase of chicken liver is inactivated rapidly and irreversibly by incubation with chloroacetyl-CoA or with bromopyruvate. Inactivation by both reagents follows saturation kinetics, indicating the formation of an E ⋯ I complex (dissociation constants of 0.36 μM for chloroacetyl-CoA...

A series of 2,6-diarylpiperidin-4-ones having electron withdrawing chloroacetyl group at the heterocyclic nitrogen were synthesized. Unambiguous characterizations of the synthesized compounds were achieved by one-dimensional (1H NMR and 13C NMR) and two-dimensional (HOMOCOSY, NOESY and HSQC spec...