Antioxidant activity of some N-heterocycles derived from 2-(1-(2-oxo-2H-chromen-3-yl)ethylidene) hydrazinecarbothioamide

Efficient and convenient synthesis of coumarin derivatives was accomplished via reactions of 2-(1-(2-oxo-2H-chromen-3-yl)ethylidene)hydrazinecarbothioamide with some carbon electrophiles, e.g. maleic anhydride, dimethyl acetylenedicarboxylate, 1,2-dichloroethane, 3′-nitro-w-bromoacetophenone, N-(4-acetylphenyl)-2-chloroacetamide, ethyl cyanoacetate/3-chlorobenzaldehyde and acetylacetone to construct some N-heterocycles such as thiazolidine, thiazole, pyrimidine and pyrazolone derivatives. The structures of all synthesized products were substantiated from their analytical and spectral data. The antioxidant activities of the synthesized compounds were examined.     

A Facile Access to Some New Pyrazole, 1,3,4-Thiadiazole,and Thiophene Derivatives via β-Ketosulfones

3-Bromoacetyl-1,5-diphenyl-1H-pyrazole-4-carbonitrile (1) reacts with sodium benzenesulfinate to give the corresponding ketosulfone 2. Treatment of 2 with hydrazonoyl chlorides 3a,b gives the 3,3′-bipyrazoles 5a,b. Ketosulfone 2 reacts also with arylidenemalononitriles to give the pyrazolylpyridones 10a,b. The reaction of compound 2 with phenylisothiocyanate and potassium hydroxide and treating intermediate with hydrazonoyl halides and with α-haloketones gives the 1,3,4-thiadiazoles 18a–c and thiophenes 21a–f, respectively.     

A Site‐Selective Doping Strategy of Carbon Anodes with Remarkable K‐Ion Storage Capacity

The limited potassium‐ion intercalation capacity of graphite hampers development of potassium‐ion batteries (PIB). Edge‐nitrogen doping is an effective approach to enhance K‐ion storage in carbonaceous materials. One shortcoming is the lack of precise control over producing the edge‐nitrogen configuration. Here, a molecular‐scale copolymer pyrolysis strategy is used to precisely control edge‐nitrogen doping in carbonaceous materials. This process results in defect‐rich, edge‐nitrogen doped carbons (ENDC) with a high nitrogen‐doping level (up to 10.5 at %) and a high edge‐nitrogen ratio (87.6 %). The optimized ENDC exhibits a high reversible capacity of 423 mAh g^?1, a high initial Coulombic efficiency of 65 %, superior rate capability, and long cycle life (93.8 % retention after three months). This strategy can be extended to design other edge‐heteroatom‐rich carbons through pyrolysis of copolymers for efficient storage of various mobile ions.     

Measurement of dose enhancement by neutron capture of boron in Cf interstitial brachytherapy

The effect of boron concentration in water on the gamma, fast and slow neutrons and alpha particles components at the central, forward and backward surfaces inside tumor phantom of 4.2 cm diameter and 4.4cm height, during brachytherapy by neutrons from ²⁵²Cf were investigated. The source was at the centre of a cubic shaped water phantom of 30 cm side. The study was carried for different concentrations of boron from H₃BO₃, Li₂B₄O₇ and H₃¹⁰BO₃. The effect of source to tumor distance on the different components of radiation was also measured. The results indicated that the use of ¹⁰B compounds enhances the damage and is recommended for successful boron neutron capture therapy (BNCT).     

Facile one‐pot syntheses of new polyfunctional pyrazolyl substituted and pyrazolofused pyridines

Ethyl 2‐cyano‐3‐(5‐chloro‐1,3‐diphenylpyrazol‐4‐yl)acrylate ( 1 ) undergoes both conjugate addition of a number of methylene‐active ethanenitriles and direct addition of other active methylene donors to the cyano carbon atom. These additions are the starting events of cascades of subsequent reactions eventually forming (i) novel polyfunctional pyrazolyl‐substituted monocyclic pyridines ( 4a , b and 6 ), (ii) 1,3‐benzothiazole and benzimidazole‐fused pyridines ( 11, 13 ) and (iii) pyrazolo[5,4‐b]pyridines ( 19b, 20 ) in one‐pot reactions in ethanolic solution containing catalytic amounts of piperidine.     

Intercomparative studies of brachytherapy techniques combined with CF Boron neutron capture therapy

In this work the depth dose distribution for γ-rays, slow and fast neutrons, nuclear recoils and -particles inside a tumor phantom filled with 100 ppm ¹⁰B in distilled water was measured. The depth dose distributions were measured and represented on three-dimensional plots when a ²⁵²Cf neutron source was situated in interstitial, surface and intracavitary brachytherapy techniques. Comparison of the three brachytherapy techniques when combined with BNCT revealed that the damage induced in the tumor by the -particles as nuclear recoils in the interstitial geometry is much more than the other two techniques.     

Potentiometric determination of antihistaminic diphenhydramine hydrochloride in pharmaceutical preparations and biological fluids using screen-printed electrode

The performance characteristic of sensitive screen-printed (SPE) and carbon paste (CPE) electrodes was investigated for the determination of diphenhydramine hydrochloride (DPH) drug in pure, pharmaceutical preparations and biological fluids. Different experimental conditions namely types of materials used to prepare the working electrode (plasticizer), titrant, pH, temperature and life time were studied. Under these conditions, the SPE shows the best performance than CPE with respect to total potential change and potential break at the end point. The SPE and CPE exhibit suitable response to DPH in a concentration range of 1.0.10^{− 2} to 1.0.10^{− 6} mol/L with a limit of detection 9.70.10^{− 7} and 9.80.10^{− 7} mol/L, respectively. The slope of the system was 55.2 ± 1.0 and 54.7 ± 1.0 mV/decade over pH range 3.0–8.0 and 3–7 for SPE and CPE, respectively. Selectivity coefficients for DPH relative to a numbers of potential interfering substances were investigated. The SPE and CPE show a fast response time of 10 and 16 s and were used over a period of 2 months with a good reproducibility. The sensors were applied successfully to determine DPH in pharmaceutical preparations and biological fluids. The results are compared with the official method.     

High UV-shielding Performance of Zinc Oxide/High-Density Polyethylene Nanocomposites

Zinc oxide/high-density polyethylene nanocomposites with high-UV-shielding efficiency were reported. Zinc oxide nanoparticles were synthesized by the homogeneous precipitation method and calcination of the precursor at different temperatures. Zinc oxide/high-density polyethylene nanocomposites were subsequently prepared from high-density polyethylene and as-prepared zinc oxide nanoparticles via melt mixing process. The structural properties of the as-prepared zinc oxide nanoparticles and nanocomposites were studied in detail using X-ray diffractometer, Fourier transform infrared spectrometer, thermogravimetry, differential scanning calorimeter, ultrasonic pulse echo technique, scanning electron microscopy, and transmission electron microscope. The optical properties of the obtained nanocomposites were shown to depend on zinc oxide particle size and content. The nanocomposite containing zinc oxide nanoparticles with an average particle size of 25.22 nm after calcination at 350°C was found to have the most optimal optical properties, namely high-visible light transparency and high-UV light shielding efficiency, which are desirable for many important applications.     

Spectroscopic and Fluorescence Studies on the Trivalent Ce,Eu,Nd and La Metal Ions Rhodamine C Florescent Dye Complexes

The four isolates solid complexes: [La(RHC)(NO₃)₂]·3H₂O, [Nd(RHC)(NO₃)₂]·4H₂O, [Eu(RHC)(NO₃)₂]·2H₂O, and [Ce(RHC)(NO₃)₂]·5H₂O that obtained by the reaction of the nitrate salts of the Ce(Ⅲ), Eu(Ⅲ), Nd(Ⅲ) and La(Ⅲ) ions and rhodamie C (RHC) ligand were interpretative using elemental analysis (C, H and N), molar conductivity, infrared, electronic, fluorescence and 1H-NMR spectra to achieve the speculated suitable formula. The low molar conductance values of the synthesized RHC complexes concluded the non-electrolytic behavior. The infrared spectra recorded the absence of stretching vibration ν(OH) of the -COOH and presence of two new vibration bands at 1 597～1 601 and 1 383～1 399 cm-1 which were assigned to ν_as(COO-) and ν_s(COO-). The difference between them revealed that the carboxylate group acts as a bidentate ligand. 1HNMR spectra of Europium and lanthanum(Ⅲ) complexes were supported the FTIR results based on the absent of proton of the carboxylic group. Therefore, the microanalytical and spectroscopic results deduced that RHC acts as a monobasic bidentate ligand, and coordinated to the central metal(Ⅲ) ions via the two oxygen atoms of deprotonated carboxylic group. Fluorescence studies were performed on the metal complexes of Ce3+, Tb3+, Th4+, Gd3+ and La3+, that referred a quenching in the fluorescene intensity of rhodamine C in the aqueous state after complexation. The antimicrobial assessment against some kind of bacteria and fungi were also checked and recorded enhancement in case of their complexes.     

Remedia Sternutatoria over the Centuries: TRP Mediation

Sneezing (sternutatio) is a poorly understood polysynaptic physiologic reflex phenomenon. Sneezing has exerted a strange fascination on humans throughout history, and induced sneezing was widely used by physicians for therapeutic purposes, on the assumption that sneezing eliminates noxious factors from the body, mainly from the head. The present contribution examines the various mixtures used for inducing sneezes (remedia sternutatoria) over the centuries. The majority of the constituents of the sneeze-inducing remedies are modulators of transient receptor potential (TRP) channels. The TRP channel superfamily consists of large heterogeneous groups of channels that play numerous physiological roles such as thermosensation, chemosensation, osmosensation and mechanosensation. Sneezing is associated with the activation of the wasabi receptor, (TRPA1), typical ligand is allyl isothiocyanate and the hot chili pepper receptor, (TRPV1), typical agonist is capsaicin, in the vagal sensory nerve terminals, activated by noxious stimulants.