Multifunctional chemicals including hydroxycarboxylic acids are gaining increasing interest due to their growing applications in the polymer industry. One approach for their production is a biological selective oxidation of polyols, which is difficult to achieve by conventional chemical catalysi...

The phthalazine carbohydrazide 2 was prepared and incorporated into the corresponding 1,2,4-triazole and carbamate derivatives. Phthalazine carboxylic acid hydrazide 2 was treated with isatine and cyclohexanone to give the corresponding hydrazone derivatives 16, 19 in good yields. Furthermore, α...

Heterocyclic compounds containing pyrazolyl-oxopropyl-quinazolin-4(3H)-one are reported to possess significant biological activity. Syntheses of 6-bromo-2-(3-chloro-2-oxopropyl)-3-(4-fluorophenyl)quinazolin-4(3H)-one 2 6-bromo-3-(4-fluorophenyl)-2-(3-hydrazinyl-2-oxopropyl)quinazolin-4(3H)-one 3...

N,N′-Diaryl-bishydrazones of [1,1′-biphenyl]-3,4′-dicarboxaldehyde, [1,1′-biphenyl]-4,4′-dicarboxaldehyde, and 4,4′-bisacetyl-1,1-biphenyl exhibited excellent antifungal activity against a broad spectrum of filamentous and non-filamentous fungi. These N,N′-diaryl-bishydrazones displayed n...

A reaction involving an efficient NBS-mediated oxidative N‒O bond formation has been established for the synthesis of 1,2,4-oxadiazoles from readily accessible N-acyl amidines. The features of this synthetic method include simplicity of operation, mild reaction conditions, short reaction times, ...

There are indications that inhibitors of the cyclooxygenase-2 (COX-2) enzyme may cause inhibition of angiogenesis, proliferation of endothelial cells and induce apoptosis in cell systems. The concentrations of inhibitors required for such effects are however much higher than those needed to inhi...

Boron trifluoride diethyl etherate catalyzes the Mannich-type reaction of 2-trifluoromethyl-4-bromoaniline and O,O-dialkylphosphite with 2-fluorobenzoaldehyde under ultrasonic irradiation to synthesize the corresponding product α-aminophosphonate. The advantages of the procedure include short r...

A novel triple reuptake inhibitor with low potential of liabilities associated with cationic amphiphilic drug (CAD) was identified following an analysis of existing drugs. Low molecular weight (MW

D3 receptor radioligands (E)-4,3,2-[11C]methoxy-N-4-(4-(2-methoxyphenyl)piperazin-1-yl)butyl-cinnamoylamides (4-[11C]MMC, [11C]1a; 3-[11C]MMC, [11C]1b; and 2-[11C]MMC, [11C]1c) were synthesized for evaluation as novel potential positron emission tomography (PET) imaging agents for brain D3 recep...

In the search for a novel serotonin 7 (5-HT7) receptor PET radioligand we synthesized and evaluated a new series of biphenylpiperazine derivatives in vitro. Among the studied compounds, (R)-1-[4-[2-(4-methoxyphenyl)phenyl]piperazin-1-yl]-3-(2-pyrazinyloxy)-2-propanol ((R)-16), showed the best co...

N-(4-[18F]-Fluoropyridin-2-yl)-N-{2-[4-(2-methoxyphenyl)piperazin-1-yl]ethyl}-carboxamides were prepared by labeling their 4-nitropyridin-2-yl precursors through nitro substitution by the 18F anion. In vitro and in vivo tests showed that the cyclohexanecarboxamide derivative is a reversible, sel...

New substituted 1-aryl-5-(1H-pyrrol-1-yl)-1H-pyrazole-3-carboxamides were synthesized by replacing the 2,4-dichlorobenzyl and cyclohexyl moieties at the 3-carboxamide nitrogen of the previously reported CB1 receptor antagonists/inverse agonists 4 and 5. Several ligands showed potent affinity for...

Long-chained ethers with relatively high relation of the number of ether groups to the chain length are interesting because of their ability to form micellar aqueous solutions even in very low concentrations. This behavior has been practically exploited in plant protection products, where micell...

We have found selective conditions for methylation of 3-trifluoromethyl-1H-pyrazol-5-ol that allowed us to obtain mono-Me-substituted N1- and O-isomers as well N1,N2-, N1,O- and N2,O-disubstituted isomers. A tautomeric structure of the parent pyrazole and its Me-substituted derivatives was inves...

An organocatalyzed asymmetric sulfa-Michael addition of thiocarboxylic acids to β-trifluoromethyl-α,β-unsaturated ketones with a chiral bifunctional amine-squaramide as the catalyst is presented. A wide range of chiral ketone compounds bearing a sulfur atom and a trifluoromethyl group at the ...

A clean, rapid and energy-efficient approach to catalyst-free one-pot synthesis of highly substituted propanamide derivatives in water was developed utilizing of the ultrasonic irradiation. The method has been successful in achieving the green chemistry objective. A catalyst-free operation, an e...

AimThe aim of the study was to compare postoperative sequelae and wound healing outcome following closure of surgical wound with either cyanoacrylate tissue adhesive or silk suture.

PurposeTo compare the clinical and histologic healing of intraoral wounds closed using No. 3-0 silk suture with that obtained with isoamyl 2-cyanoacrylate glue.

The chalcone compound (2E)-1-(4-aminophenyl)-3-phenyl-prop-2-en-1-one of chemical formula C15H13NO was synthesized and structurally characterized using Nuclear Magnetic Resonance (NMR). The spectroscopy investigation has been carried out by Fourier Transform Raman (FT-Raman), Fourier Transform i...

N,N′-Bis(4-aminophenyl)1,4-quinonenediimine doped with silicotungsten polyacid were investigated by Raman, IR and UV–Vis absorption methods and the results analyzed based on numerical approaches. In this aim, density functional theory (DFT) calculations were performed to optimize the geometry ...