In this paper, 2-hydroxyethyl dibutyldithiocarbamate (HEBTC) containing thione and hydroxy groups was synthesized and introduced as a new flotation surfactant for recovering chalcopyrite. HEBTC’s chemical reactivity and dispersion performances were studied via DFT calculations and surface tensi...

A series of novel β2-adrenoceptor agonists with a 5-(2-amino-1-hydroxyethyl)-8-hydroxyquinolin-2(1H)-one moiety was designed, synthesized and evaluated for biological activity in human embryonic kidney 293 cells and isolated guinea pig trachea. Compounds 9g and (R)-18c exhibited the most excell...

5-Lipoxygenase (5-LOX) is a key enzyme involved in the biosynthesis of pro-inflammatory leukotrienes, leading to asthma. Developing potent 5-LOX inhibitors especially, natural product based ones, are highly attractive. Coumaperine, a natural product found in white pepper and its derivatives were...

Publisher SummaryThe oxidation of phenols has many different aspects. Oxidative coupling, the formation of cyclohexadienones, and conversion to quinones and other carbonylic and transformation products (other than those obtained by electrophilic substitution or rearrangement of phenyl esters) ar...

The present study compares, theoretically and experimentally, the antioxidant power of isoespintanol (2-isopropyl-3,6-dimethoxy-5-methylphenol) isolated from the leaves of Oxandra cf. xylopioides, with its biosyntetic analogue thymol (2-isopropyl-5-methylphenol). Calculations based on the densit...

Chlorocarbenium salts 2a-d of the Vilsmeier-Arnold type react with the silylated isocyanuric acid 3 to give 1-oxa-3-azabutatrienium salts 1 under mild conditions. From reactions of diarylchloromethenium salts 2h-1 with 3 and ketones or tertiary carboxamides high yields of 2-azaallenium salts 9 w...

6/6,7-Substituted 3-formylchromones (9a–e) react with 2 equivalents of 2-phenyl-4-dimethylamino-1-thia-3-azabuta-1,3-diene (10) or thiobenzamide (11) in refluxing toluene to furnish novel substituted 3-(5-phenyl-3H-[1,2,4]dithiazol-3-yl)chromen-4-ones (12a–e). However, reactions of substituted...

Various novel 10-alkyl-2-deoxo-2-methylthio-5-deazaflavins have been synthesized by reaction of 6-(N-alkylanilino)-2-methylthiopyrimidin-4(3H)-ones with Vilsmeier reagent. The similar 2-(N-substituted amino) derivatives were prepared by nucleophilic replacement reaction of the 2-methylthio moiet...

3-Hydroxytyramine (dopamine) appears to be an effective drug for the treatment of cardiogenic, traumatic and hemorrhagic shock states because it restores systemic pressure while it increases the blood flow to the kidney, gastrointestinal tract and coronary circulations.Concomitant use of alpha a...

1.1. The inhibitory activities of γ-aminobutyric acid, 3-hydroxytyramine, imidazoleacetic acid and homotaurine upon the slowly adapting neurones of four species of crayfish have been compared.2.2. 3-Hydroxytyramine is active only on Pacifastacus leniusculus and Procambarus clarkii and is withou...

Six male subjects were infused with 104·6 μc 3-hydroxytyramine-2-C14 (dopamine). The hydroxytyramine was dissolved in 1000 ml physiological saline and infused at a constant rate for 4 hr. Urine was collected at the end of the infusion period and at 2-hr intervals for the first 4 hr post infusi...

A phenotypic screen of a compound library for antiparasitic activity on Trypanosoma brucei, the causative agent of Human African Trypanosomiasis (HAT), led to the identification of N-(2-aminoethyl)-N-phenyl benzamides as a starting point for hit-to-lead medicinal chemistry. Eighty two analogues ...

Synthesis and vasodilatory activity of some amide derivatives of 6-(4-carboxymethyloxyphenyl)-4,5-dihydro-3(2H)-pyridazinone are reported. An effect of substitution at 2-position of pyridazinone ring on vasodilatory potential has also been explored. The most active compound 6-[4-(2-oxo-2-pyrroli...

Dipeptidyl peptidase IV (DPP-4) inhibition is suitable mechanism for once daily oral dosing regimen because of its low risk of hypoglycemia. We explored linked bicyclic heteroarylpiperazines substituted at the γ-position of the proline structure in the course of the investigation of l-prolylthi...

A series of (2R,3S)-2-(2,4-difluorophenyl)-3-(5-{2-[4-aryl-piperazin-1-yl]-ethyl}-tetrazol-2-yl)-1-[1,2,4]-triazol-1-yl-butan-2-ol (11a–n) and (2R,3S)-2-(2,4-difluorophenyl)-3-(5-{2-[4-aryl-piperazin-1-yl]-ethyl}-tetrazole-1-yl)-1-[1,2,4]-triazol-1-yl-butan-2-ol (12a–n) has been synthesized. T...

Acid promoted cyclisation of homochiral (R)-N-(3,4-dimethoxyphenethyl)-halostachine proceeds with almost total racemisation to yield 1-phenyl-N-methyl-1,2,4,5-tetrahydrobenz[d]azepine (e.e. 6%). Coordination of the cyclisation precursor to the tricarbonylchromium(0) moiety renders the cyclisatio...

The stereochemistry of 2- and 4-phenyl-6,7-dimethoxy-3-methyl-3,4-dihydro-2H-1,3-benzothiazine (2,6) has been studied by 1H, 13C NMR spectroscopy and X-ray diffraction. Crystals of compound 2 (C17H19NO2S) are monoclinic, space group P21/n, with a = 11.428(1), b = 10.048(1), c = 14.161(2) Å, ß = ...

The synthesis of some Nmethyl, N-alkyl derivatives of (±)α-phenyl-β-(3,4-dimethoxy)- and (±)α-phenyl-β-(3,4-dihydroxy)-phenethylamines was achieved. These compounds were shown to bear certain structural features of acetylcholine (ACh), as well as phencyclidine (PCP). The latter was reporte...

Monoamine oxidase (MAO) inhibitors were the first antidepressant drugs to be prescribed and are still used today with great success, especially in patients resistant to other antidepressants. In this study, we evaluated the MAO inhibitory properties and the potential antidepressant action of 2-(...

Some derivatives of α-phenyl-β-(3,4-dimethoxy)phenethylamine that might bear a certain conformational resemblance to choline were prepared. The in vitro inhibition of choline acetyltransferase from Torpedo electric organ was investigated. These compounds gave variable degrees of inhibition; th...