The pharmacokinetics (PK) and metabolism of 3,4-dichlorophenyl-propenoyl-sec.-butylamine (3,4-DCPB), a novel antiepileptic drug, were investigated after its oral administration to rats (100 mg/kg) by HPLC. The absorption and elimination of 3,4-DCPB were rapid. 3,4-DCPB was found to undergo exten...

During our research using a high-throughput screening system for discovery of a new class of human liver glycogen phosphorylase a (hLGPa) inhibitors, a series of 3-(3,4-dichlorophenyl)acrylamide derivatives were synthesized, and their inhibitory activities toward hLGPa were evaluated. Among the ...

Herein, we report synthesis and evaluation of new twenty-eight pyrazinyl ureas against β amyloid (Aβ)-induced opening of mitochondrial permeability transition pore (mPTP) using JC-1 assay which measures the change of mitochondrial membrane potential (ΔΨm). The neuroprotective effect of seven...

Three novel mononuclear complexes, [MⅡ(L)2·2H2O], (M = Cu, Ni or Cd; HL = 4-(3,4-dichlorophenyl)piperazine-1-carboxylic acid)were synthesized and structurally determined by single-crystal X-ray diffraction. Molecular docking study preliminarily revealed that complex 1 had potential urease inhi...

Sixteen substituted styryl 3,4-dichlorophenyl ketones [(2E)-1-(3,4-dichlorophenyl)-3-phenyl-2-propen-1-ones] were synthesized using eco-friendly benign stereoselective crossed-aldol reaction. They are characterized by their analytical, infrared, NMR and mass spectral data. The insect antifeedant...

The novel triple reuptake inhibitor (S)-4-(1-(3,4-dichlorophenyl)-2-methoxyethyl)piperidine monohydrochloride 1 possesses a unique 2-phenyl-2-(piperidin-4-yl)ethanol moiety with a stereogenic center at the benzyl position. To synthesize 1 as the (S)-isomer, three possible routes were investigate...

The compound 3,4‑dichlorophenyl‑propenoyl‑sec.‑butylamine (3,4‑DCPB) is an antiepileptic drug. The purpose of the present research was to identify cytochrome P450 (CYP450) responsible for the metabolism of 3,4‑DCPB and evaluate the effects of 3,4‑DCPB on the activities of CYP450 enzymes. 3,4‑DCP...

High expression of the aldo-keto reductase enzyme AKR1C3 in the human prostate and breast has implicated it in the development and progression of leukemias and of prostate and breast cancers. Inhibitors are thus of interest as potential drugs. Most inhibitors of AKR1C3 are carboxylic acids, whos...

In this communication, we synthesized a series of twenty four novel 3-(4-(substitutedsulfonyl)piperazin-1-yl)benzo[d]isoxazole analogues, characterized using various spectroscopic techniques and evaluated for their in vitro anti-tubercular activity against Mycobacterium tuberculosis (MTB) H37Rv ...

This study describes the development of a series of 1-arylsulfonyl-6-(N-hydroxyacrylamide)tetrahydroquinolines, potent histone deacetylase (HDAC) inhibitors which are cytotoxic to PC-3 cells. (E)-N-hydroxy-3-(1-(4-methoxyphenylsulfonyl)-1,2,3,4-tetrahydroquinolin-6-yl)acrylamide (11) exhibits ma...

In our previous study, we reported a series of 1-hydroxy-2-phenyl-1H-imidazole-5-carboxylic acid derivatives that presented excellent in vitro xanthine oxidase inhibitory potency. As a continuation study, a series of 1-hydroxy-2-phenyl-1H-imidazole derivatives containing a pyridine moiety (4a-g ...

Enantiomerically pure precursors of β-blockers (propranolol, alprenolol and 1-(isopropylamino)-3-p-methoxy-phenoxy-2-propanol) were synthesized. Key step is the lipase-catalyzed kinetic resolution of rac-3-hydroxy esters either by O-acylation using vinyl acetate or by hydrolysis of the ester gr...

A flow-injection analytical method for the determination of hydrochlorothiazide is presented. The method is based on the chemiluminescence reaction of hydrochlorothiazide with cerium(IV) in sulphuric acid, sensitized by the fluorescent dye rhodamine 6G. The proposed procedure allows quantitation...

We report an investigation of the effect of benzil and cobalt stearate on the degradation behaviour of LDPE films. Thin films (70 μ) containing these additives were prepared by sheeting process. The effect of heating, exposure to UV-B and natural weathering of LDPE films in the presence/absence...

The layered double hydroxides (LDH) Mn2Al-LDH-stearate and Co2Al-LDH-stearate were prepared by a surfactant-assisted intercalation of the corresponding precursor LDH-CO3 forms. These compounds were evaluated as potential photodegradant additives in low density polyethylene films with a thickness...

In this paper, the study investigates the combined application of water additive and metal-based additive in the biodiesel-diesel blend fuel. Varied mixtures of biodiesel- diesel (B5), water (i.e. 2%, 4% and 6% wt.) and cerium oxide (CeO2) nanoparticles (90 ppm) components are compared with pure...

Improving fuel combustion in engines and consequently reducing environmentally-unfavorable emissions is of prominent importance in addressing some of the main challenges of the current century, i.e., global warming and climate change. Fuel additives are considered as efficient way for improving ...

The thermal behavior and decomposition of Ce-butanoate monohydrate (Ce(C3H7CO2)3·H2O), Ce-pentanoate (Ce(C4H9CO2)3) and Ce-hexanoate (Ce(C5H11CO2)3) were studied in a flow of argon while heating at 5 °C/min. By means of several techniques such as simultaneous TG-DTA, FTIR evolved gas analysis,...

The effect of neodymium stearate (NdSt) on cure and mechanical properties of expoxidized natural rubber with 25 mol.% epoxidation (ENR25) was studied in the concentration range of 0 to 2 phr, and the relationship between structure and mechanical properties of ENR25 vulcanizates was also discusse...

Stearic acid-capped cerium borate composite nanoparticles, abbreviated as SA/CeBO3, were prepared by hydrothermal method. The morphologies, element compositions, size distributions, crystal and chemical structures, hydrophobic characteristics, of SA/CeBO3 were characterized by scanning electron ...