The reaction of N,N-disubstituted benzamide derivatives 1 with lithium and a catalytic amount of naphthalene (4 mol %) in the presence of carbonyl compounds (Barbier-type conditions) led to the formation of the corresponding 3,4-dihydro-4-substituted benzamides 2. The presence of a 4-tert-butyl ...

A quick, miniaturized and on-line method has been developed for the determination in water of the predominant homologue of benzalkonium chloride, dodecyl dimethyl benzyl ammonium chloride or lauralkonium chloride (C12-BAK). The method is based on the formation of an ion-pair in both in-tube soli...

A simple reversed-phase HPLC method has been developed for the determination of cholesteryl 14-methylhexadecanoate (CMH) in the blood serum. Lipids are extracted from 0.1 ml of blood serum and after centrifugation, the extract is chromatographed and individual cholesteryl esters, including CMH a...

The Lewis acid-catalyzed Diels–Alder reactions of suitably substituted imidazole-2-thiones with dienes were studied. It was found that the electron density of the imidazole core influenced the reaction, since electron withdrawing groups led to the novel spiro-derivatives 2 whereas electron dona...

A new series of amino-3,5-dicyanopyridines (3–28) as analogues of the adenosine hA2B receptor agonist BAY60-6583 (compound 1) was synthesized. All the compounds that interact with the hA2B adenosine receptor display EC50 values in the range 9–350 nM behaving as partial agonists, with the only ...

Friedländer condensation of 2-amino-6-chlorochromone-3-carboxaldehyde (1) with 4-hydroxycoumarin (2) under basic conditions afforded 10-chloro-6H,8H-dichromeno[2,3-b:3′,4′-e]pyridine-6,8-dione (3) (CDPD). Structure of CDPD was deduced based on its correct elemental analysis and spectral data (...

A variety of5-alkylidene-4-chloro-5H-1,2,3-dithiazoles (9–25) have been prepared from4-chloro-5H-1,2,3-dithiazolium chloride, active methylene compounds, and pyridine. The reactions with ethyl nitroacetate ((Z) > (E)), ethyl 3-nitrobenzoylacetate ((E) > (Z)), ethyl 2-fluorobenzoylacetate ((E) >...

A series of coumarins incorporating hydroxy-, chloro- and/or chloromethyl-moieties in positions 3-, 4-, 6- and 7- of the heterocyclic ring were investigated for the inhibition of the zinc enzyme carbonic anhydrase (CA, EC 4.2.1.1). These coumarins were very weak or ineffective as inhibitors of t...

A series of 3-aryl-4-hydroxycoumarin derivatives was synthesized with the aim to find out the structural features for the MAO inhibitory activity and selectivity. Methoxy and/or chloro substituents were introduced in the 3-phenyl ring, whereas the position 6 in the coumarin moiety was not substi...

4-Chloro-3-(trifluoroacetyl)coumarin was synthesized for the first time via direct TMSCl-mediated acylation of 4-hydroxycoumarin with TFAA followed by the treatment with POCl3. The reaction of 4-chloro-3-(trifluoroacetyl)coumarin with commercially available anilines is a two-step method, which a...

Crystal structures of thiosemicarbazones prepared from 3- and 4-formylpyridine and 3- and 4-acetylpyridine are included along with their UV spectra. 4-Formylpyridine thiosemicarbazone has the following structural properties: monoclinic, P21/n, a=7.2420(5), b=13.961(1), c=8.415(1)Å,β=90.90(1)°...

Pyruvaldehyde mixed bis(thiosemicarbazones) have been prepared in which the two thiosemicarbazone moieties have different N(4)-substituents. The mixed bis(thiosemicarbazones) and their copper(II) and nickel(II) complexes have been characterized with IR, electronic, mass, 1H NMR (Ni) and EPR (Cu)...

Bis(thiosemicarbazones) and their copper (Cu) complexes possess unique anti-neoplastic properties. However, their mechanism of action remains unclear. We examined the structure–activity relationships of twelve bis(thiosemicarbazones) to elucidate factors regarding their anti-cancer efficacy. Im...

Six tetradentate bis-thiosemicarbazone ligands formed by condensation of pyruvaldehyde with 4-(aryl) thiosmicarbazides and their Ru(II) complexes are reported. The complexes are of formula [Ru(PPh3)2(L)], where L is the dianionic form of the bis-thiosemicarbazone ligands. X-ray crystal structure...

Background. Copper-62 (II)-pyruvaldehyde bis(N4-methyl-thiosemicarbazone) (PTSM) has been proposed for cardiac imaging with positron emission tomography (PET). This study evaluated the agreement between Cu-62-PTSM and coronary angiography in the detection of occlusive coronary artery disease. Th...

4-S-Cysteinylphenol (4-CP) has been shown to exert selective toxicity to melanocytes, causing growth inhibition of experimental malignant melanoma. 4-S-Cysteinyl-[U-14C]phenol (4-[U-14C]CP) has now been synthesized by reaction of [U-14C]phenol with excess l-cystine in HBr. After crystallization ...

BackgroundCatechol-O-methyltransferase (COMT) metabolizes dopamine. The COMT Val158Met polymorphism influences its activity, and multiple neural correlates of this genotype on dopaminergic phenotypes, especially working memory, have been reported. COMT activity can also be regulated pharmacologi...

The determination of phenoxy ester herbicides was carried out by high-performance liquid (HPLC) and gas chromatography (GC) and their identification by GC—MS spectrometry. Standards of herbicide esters were obtained from the appropriate acid and a suitable alcohol, mainly 2-butoxyethyl, isoocty...

Ammonium ionic liquids with the 4-chloro-2-methylphenoxyacetate anion were synthesized and characterized. Physicochemical properties, such as thermal stability, phase transition temperatures, viscosity, density, refractive index, as well as surface activity and herbicidal activity were determine...

Vinyl triflates react with β-substituted-α,β-unsaturated aldehydes, ketones, and esters in the presence of catalytic amounts of Pd(OAc)2 and an exeess of KOAc, omitting phosphine ligands, to give vinylic substitution products in good to high yield with high regioselectivity. The added vinyl u...