Isolation of a urease from watermelon seeds and the study of its properties

The enzyme urease has been isolated from the seeds of the watermelon of the Ogonek variety and has been characterized. The molecular weight of a rechromatographed sample of the enzyme has been determined as 480,000. The pH dependence of the activity of the urease and the kinetic parameters of the enzyme have been studied.All-Union Scientific-Research Institute of the Chemistry and Technology of Drugs, Khar'kov. Vitaminy Scientific-Production Amalgamation, Moscow. Translated from Khimiya Prirodnykh Soedinenii, No. 5, pp. 624–628, September–October, 1983.     

Synthesis of New Heteroatomic Podands from Ethyl 2-[(2-Aminophenylamino)Methylidene]-3-Oxoalkanoates and Thiophene-2,5-Dicarboxaldehyde

Condensation of two moles of ethyl 2-[(2-aminophenylamino)methylidene]-3-oxo-3-(polyfluoroalkyl)propionates with 2,5-thiophene-dicarboxaldehyde results in new heteroatomic podands. X-ray data showed that in the solid state these molecules arrange in two independent chelating fragments of b-amino enone type, thiophene fragment being a spacer.     

A Convenient Approach to 4,7‐Dihydrotetrazolo [5,1‐c][1,2,4]triazine Synthesis

Azo coupling of 1,3‐dicarbonyl compounds with tetrazolyl‐5‐diazonium chloride is used to develop a convenient one‐step procedure for the synthesis of 4,7‐dihydrotetrazolo[5,1‐c][1,2,4]triazines. In contrast to nonfluorinated analogs, 7‐hydroxy‐7‐polyfluoroalkyl‐4,7‐dihydrotetrazolo[5,1‐c][1,2,4]triazines undergo a ring‐chain isomerism resulting from the cleavage at the C7―N7a bond. A distinctive feature of nonfluorinated 4,7‐dihydrotetrazolo[5,1‐c][1,2,4]triazines is the possibility to dehydration, which is accompanied by an azide rearrangement due to the tetrazole ring cleavage with the formation of tetrazolo[1,5‐b][1,2,4]triazines.     

A concise approach to CF3-containing furan-3-ones, (bis)pyrazoles from novel fluorinated building blocks based on 2,3-butanedione

1,1,1-Trifluoro-4,5,5-trimethoxyhex-3-en-2-one and lithium (2Z)-1,1,1-trifluoro-5,5-dialkoxy-4-oxohex-2-en-2-olate were synthesized for the first time via direct trifluoroacetylation of 2,3-butanedione acetal derivatives. A simple and effective approach to acetal or acyl substituted CF₃-pyrazoles, 5,5′-bis(trifluoromethyl)-3,3′-bipyrazole, and, to 5-trifluoromethylfuran-3-ones is presented.     

The Effectiveness of Glycerol Solutions for Optical Clearing of the Intact Skin as Measured by Confocal Raman Microspectroscopy

Optics and Spectroscopy - The effect of glycerol solutions of different concentrations and exposure times on the optical clearing efficiency in intact pig skin has been studied in the analysis of...     

A corresponding states principle-based equation for the surface tension of Alkenes

This study presents a new formula for the surface tension prediction of alkenes. As a first step, an analysis of the available data of the experimental surface tension data for alkenes was performed. The experimental data were collected, after a careful literature survey, for the following pure fluids: propene, 1-hexene, 1-heptene, 1-octene, 1-decene, 1-tetradecene, and 1-pentadecene. Then, the experimental data were regressed with the most reliable semi-empirical correlating methods based on the corresponding state theory existing in the literature. As a final step, an analysis of the available data of the experimental surface tension data for alkenes was performed starting from the two recently proposed equations for the prediction of the surface tension of refrigerants based on the corresponding states principle. To minimize the deviation between the predicted data and the experimental data and to find the optimal equation coefficients for experimental data regression, a (μ + λ)-evolution strategy was adopted. The analysis showed that the equation that gave the best results for the prediction of the surface tension of alkenes was the one with a very limited number of parameters. The finally proposed equation is very simple and gives a noticeable improvement with respect to the existing equations. It is based on the corresponding state principle, containing the acentric factor, the critical temperature, and pressure.     

Solid–liquid equilibria for the dimethyl ether + carbon dioxide binary system

A recently built experimental setup was employed for the estimation of the solid–liquid equilibria of alternative refrigerants systems. The behavior of dimethyl ether (DME) + carbon dioxide was measured down to temperatures of 131.6 K. To confirm the reliability of the apparatus, the triple point of the DME was measured. The triple point data measured revealed a good consistency with the literature. The results obtained for the mixtures were corrected by the Rossini method and interpreted by means of the Schröder equation.     

Polyvinyl Alcohol–Pectin Cryogel Films for Controlled Release of Enrofloxacin

The release of enrofloxacin entrapped in polyvinyl alcohol (PVA) cryogel at pH?5.5 showed a first-order kinetic, releasing 69.7% of the antibiotic after 4.5?h at 37?°C. In order to slow down the fluoroquinolone release rate, high-methoxylated pectin was added into the cryogel (PVA?CP). A film containing 1.0% (w/v) HM pectin and 5.0???g/ml enrofloxacin released only 3.7% of the antibiotic after 4.5?h. Since the FTIR spectrum showed that most of the interactions between PVA?CP matrix and enrofloxacin were due to polar groups (carboxylate and amine), a two-layer film system was designed to modulate the releasing rate of the drug. The top film equilibrated with 0.75 or 1.5?M NaCl release up to 41.9% and 89.0% of the enrofloxacin in 4?h, respectively. The release rate of enrofloxacin was found dependent on NaCl concentration in the upper gel layer. The two-layer cryogel system showed attractive features for transcutaneous antibiotic delivery.     

Dinuclear copper(ii) complex with novel N,N’,N”,O-tetradentate Schiff base ligand containing trifluoromethylpyrazole and hydrazone moieties

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Synthesis of 4-Aminopyrazol-5-ols as Edaravone Analogs and Their Antioxidant Activity

One of the powerful antioxidants used clinically is Edaravone (EDA). We synthesized a series of new EDA analogs, 4-aminopyrazol-5-ol hydrochlorides, including polyfluoroalkyl derivatives, via the reduction of 4-hydroxyiminopyrazol-5-ones. The primary antioxidant activity of the compounds in comparison with EDA was investigated in vitro using ABTS, FRAP, and ORAC tests. In all tests, 4-Amino-3-pyrazol-5-ols were effective. The lead compound, 4-amino-3-methyl-1-phenylpyrazol-5-ol hydrochloride (APH), showed the following activities: ABTS, 0.93 TEAC; FRAP, 0.98 TE; and ORAC, 4.39 TE. APH and its NH-analog were not cytotoxic against cultured normal human fibroblasts even at 100 μM, in contrast to EDA. According to QM calculations, 4-aminopyrazolols were characterized by lower gaps, IP, and η compared to 4-hydroxyiminopyrazol-5-ones, consistent with their higher antioxidant activities in ABTS and FRAP tests, realized by the SET mechanism. The radical-scavenging action evaluated in the ORAC test occurred by the HAT mechanism through OH bond breaking in all compounds, directly dependent on the dissociation energy of the OH bond. All the studied compounds demonstrated the absence of anticholinesterase activity and moderate inhibition of CES by some 4-aminopyrazolols. Thus, the lead compound APH was found to be a good antioxidant with the potential to be developed as a novel therapeutic drug candidate in the treatment of diseases associated with oxidative stress.